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Journal articles on the topic '4-Amino Quinazoline'

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Published: 9 March 2023
Last updated: 10 March 2023

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1

Widiyana, Anita Puspa. "COMPUTATION DESIGN OF QUINAZOLINE-4(3H)-ON DERIVATIVES AS CYCLOOXYGENASE-2 (COX-2) INHIBITOR." Jurnal Farmasi Sains dan Praktis 7, no. 2 (November 1, 2021): 163–70. http://dx.doi.org/10.31603/pharmacy.v7i2.4827.

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The 3-(benzylideneamino)-2-(2,4-dichlorophenyl)-quinazoline-4(3H)-ones (BDCQ) are compounds developed as anticancer drugs and quinazolines. The activity and bioavailability of BDCQ derivatives as anticancer compounds that inhibit COX-2 can be predicted by computer programs and online servers. Substituents are added at positions 2 and 3 to the quinazoline-4(3H)-on ring, such as -H, -NO2, -OCH3, -N(CH3)2, -SO2NH2, -OH, and –OCH3. QSAR as COX-2 inhibitor analysis was performed by SPSS Ver. 21 software. Lipinski’s rule of five for determining bioavailability is performed by an online server at http://ilab.acdlabs.com. The best QSAR equation used to predict the COX-2 inhibitors from these compounds is RS-pred = 0.372 Log P + 0.014 MR + 0.979 Etot – 4.859, with n= 12, R = 0.998; SE = 0.356, F = 805.252 and sig = 0.001. Six compounds were predicted to have good oral bioavailability, such as 3-(benzylideneamino)-2-(2,4-dichlorophenyl)quinazoline-4(3H)-one, 2-(2,4-dichlorophenyl)-3-((2-nitrobenzylidene)amino)quinazoline-4(3H)-one, 2-(2,4-dichlorophenyl)-3-((3-nitrobenzylidene)amino)quinazoline-4(3H)-one, 2-(2,4-dichlorophenyl)-3-((2-methoxybenzilidene)amino)quinazoline-4(3H)-one, 2-(2,4-dichlorophenyl)-3-((3-methoxybenzylidene)amino)quinazolin-4(3H)-one, and 2-(((2-(2,4-dichlorophenyl)-4-oxoquinazolin-3(4H)-yl)imino)methyl)- benzenesulfonamide. This research can be used as an in vitro and in vivo study for BDCQ derivatives as anticancer drugs.
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2

Peter Osarodion Osarumwense, Mary Olire Edema, and Cyril Odianosen Usifoh. "Synthesis and antibacterial activities of quinazolin-4(3h)-one, 2-methyl-4(3h)-quinazolinone and 2–phenyl-4(3h)-quinazolinone." International Journal of Biological and Pharmaceutical Sciences Archive 1, no. 2 (April 30, 2021): 077–84. http://dx.doi.org/10.30574/ijbpsa.2021.1.2.0027.

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Background: Quinazoline and quinazolinone scaffolds represent an important class of biologically active nitrogen heterocyclic compounds. Many marketed drugs are based on these moieties. A diverse range of molecules with quinazoline/quinazolinone moieties have been reported to exhibit broad spectrum of biological activities Objective: This study is aimed at the synthesis of these quinazolinone derivatives, quinazolin-4(3H)-One, 2-Methyl-4(3H)-quinazolinone and 2–Phenyl-4(3H)-quinazolin-4(3H)–one and evaluate them for their antibacterial activities. Method: The consolidation of 2-amino-methyl-4-methoxybenzoate with acetic anhydride produced the cyclic compound 2-methyl-4, 5-disubstituted-1, 3-benzo-oxazine-4-one which also produce a novel 2,3-disubstituted quinazolin-4 ones via the reaction with hydrazine hydrate. The quinazolinone derivatives quinazolin-4(3H)-One, 2-Methyl-4(3H)-quinazolinone and 2–Phenyl-4(3H)-quinazolin-4(3H)–one were evaluated pharmacologically for their in vivo analgesic activities by acetic acid induced writhing in mice. The compounds synthesized were assuredly validated by means of Infrared, Nuclear Magnetic Resonance (1H and 13C), Gas Chromatography Mass Spectrophotometer and Elemental analysis. The synthesized compounds were tested for their antibacterial activity.Compounds 1,2 and 3 showed significant antibacterial activities. Discussion: Compound 1 was identified by the absence of methyl group and the presence of methyl group for compound 2. The test analysed compounds exhibited significant antibacterial activities. The compounds synthesized exhibited promising antibacterial activities against the tested organisms. Conclusion: The compounds have high antibacterial activities. Compound 2 has a higher activity compared to Compound 1 and 3. Compound 2 has a higher antibacterial against Escherichia coli, Klebsiella pneumonia and Pseudomonas aeuriginosa
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3

Martynenko, Yulya, Oleksii Antypenko, Inna Nosulenko, Galina Berest, and Sergii Kovalenko. "Directed Search of Anti-inflammatory Agents Among (3HQuinazoline- 4-ylidene)hydrazides of N-protected Amino acids and their Heterocyclization Products." Anti-Inflammatory & Anti-Allergy Agents in Medicinal Chemistry 19, no. 1 (February 24, 2020): 61–73. http://dx.doi.org/10.2174/1871523018666190115092215.

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Background: (Quinazoline-4-ylidene)hydrazides are valued intermediates in modern organic chemistry, as they are commonly used for the synthesis of substituted [1,2,4]triazolo[1,5-c]quinazolines. Objective: Unknown N-acyl-2-([1,2,4]triazolo[1,5-c]quinazoline-2-yl)-alkyl-(alkaryl-, aryl-) amines were synthesized and evaluated for anti-inflammatory potential. Methods: The peculiarities of the synthesized compounds structures were studied by IR-, NMR spectroscopy and chromatography-mass spectrometry and were discussed in detail. Probable molecular mechanisms of activity (inhibition of COX-1 and COX-2) were predicted due to molecular docking. Anti-inflammatory activity of synthesized compounds was determined by their ability to reduce the formalin-induced paw edema in rats. Diclofenac sodium was used as reference drug. Results: In this study, the synthesis of N-acetyl-(benzoyl)-2-([1,2,4]triazolo[1,5-c]quinazolinе- 2-yl)alkyl-(aralkyl-, aryl-)amines, using (3H-quinazoline-4-ylidene)hydrazides of Nprotected amino acids or 4-hydrazinoquinazoline and N-prorotected amino acids as starting compounds was developed. It was established that the reaction of (3H-quinazoline-4- ylidene)hydrazides of Boc-amino acids occurred with the formation of N-acetyl-substituted triazoloquinazolines. High anti-inflammatory activity was detected for unknown (3Hquinazoline- 4-ylidene)hydrazides Boc-amino acids (1.13-1.15) and N-acetyl-(benzoyl)-2- ([1,2,4]triazolo[1,5-c]quinazoline-2-yl-)aralkyl-(aryl-)amines (3.2, 3.3, 3.11, 3.12), using the experimental formalin test. Conclusion: The conducted SAR-analysis allowed to detect critical fragments. Namely, the Boc-aminoaralkyl-(aryl-)acid residue in (3H-quinazoline-4-ylidene)hydrazides (1.13- 1.15), benzyl and phenyl linker groups in N-acetyl-(benzoyl)-2-([1,2,4]triazolo[1,5- c]quinazoline-2-yl-)aralkyl-(aryl-) amines (3.2, 3.3, 3.11, 3.12) are believed to be substantial for anti-inflammatory activity.
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4

Srivastav, Manish, MD Salahuddin, and S. M. Shantakumar. "Synthesis and Anti-inflammatory Activity of Some Novel 3-(6-Substituted-1, 3-benzothiazole-2-yl)-2-[{(4-substituted phenyl) amino} methyl] quinazolines-4 (3H)-ones." E-Journal of Chemistry 6, no. 4 (2009): 1055–62. http://dx.doi.org/10.1155/2009/507052.

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A series of novel 3-(6-substituted-1, 3-benzothiazole-2-yl)-2-[{(4-substituted phenyl) amino} methyl] quinazolines-4(3H)-ones were synthesized by treating 2-(chloromethyl)-3-(6-substituted-1, 3-benzothiazole-2-yl) quinazoline-4-(3H)-one (IIa-d) with various substituted amine. The compounds (IIa-d) prepared by treating 2-[(chloroacetyl) amino] benzoic acid with different 2-amino-6-substituted benzothiazole. Elemental analysis, IR,1HNMR and mass spectral data confirmed the structure of the newly synthesized compounds. Synthesized quinazolines-4-one derivative were investigated for their anti-inflammatory and antibacterial activity.
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5

Bhavesh, Amrute B., Amrutkar D. Rakesh, and Tambe R. Santosh. "Design and Molecular Docking Studies of Some 2,3 Di-Substituted Quinazolin-4-One Analogues Against Staphylococcus aureus UDG." Current Computer-Aided Drug Design 16, no. 4 (September 3, 2020): 402–6. http://dx.doi.org/10.2174/1573409915666190916100437.

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Background: In this present investigation, some 2, 3 disubstituted-quinazolin-4-one derivatives are designed and docked against chain A and chain B of (3WDF) receptor. Methods: The heterocyclic fused rings quinazolinone have drawn a great attention owing to their expanded applications in the field of pharmaceutical chemistry. The diverse range of molecules with quinazoline/quinazolinone moieties have been reported to exhibit a broad spectrum of biological activities. Results: The results designate that the quinazolinone ring forms hydrophobic and hydrogen bond contacts with ASN 127 A, ALA 126 A, and SER 83 B, SER 183 B amino acid residue. Conclusion: : Molecular docking is safe and straightforward to use tool which facilitates in investigating, interpreting, enplaning and identification of molecular properties using 3D structures.
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6

Špirková, Katarína, and Štefan Stankovský. "Annelation to the Quinazoline Ring. Preparation of Some Substituted 2H-Imidazo- and 2,3-Dihydropyrimido[1,2-c]quinazolines." Collection of Czechoslovak Chemical Communications 61, no. 6 (1996): 957–61. http://dx.doi.org/10.1135/cccc19960957.

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Preparation of some substituted 2H-imidazo[1,2-c]quinazolin-3-ones (2a-2f) and 2,3-dihydropyrimido[1,2-c]quinazolin-4-ones (3a-3c) by reaction of corresponding 3H-quinazoline-4-thiones (1a-1d) with amino acid esters is described. IR, 1H NMR and 13C NMR spectra of the compounds synthesized are presented.
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7

Abdel-Megeed, Mohamed Farghali, and Abderrahman Teniou. "Synthesis of some 3-substituted 4(3H)-quinazolinone and 4(3H)-quinazolinethione derivatives and related fused biheterocyclic ring systems." Collection of Czechoslovak Chemical Communications 53, no. 2 (1988): 329–35. http://dx.doi.org/10.1135/cccc19880329.

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The reactions of 2-phenyl-4(3H)-quinazoline, 2-phenyl-3-amino-4(3H)-quinazolinone, and corresponding thiones with phenyl isocyanate or phenyl isothiocyanate were investigated. The resulting urea and thiourea quinazolinone or quinazolinethione derivatives reacted with hydrazine hydrate, phenylhydrazine, and urea or thiourea to form fused biheterocyclic ring systems with potential biological activities. The products were identified by IR, 1H NMR, and mass spectroscopy.
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8

Javzan, S., D. Selenge, Y. Jamyansan, J. Nadmid, and Yu Ouynbileg. "Alkaloids from cultivated plant of Peganum harmala L." Mongolian Journal of Chemistry 12 (September 24, 2014): 113–16. http://dx.doi.org/10.5564/mjc.v12i0.184.

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Alkaloids such as 1H-cyclopenta(b) quinoline, 2.3.5.6.7.8-hexahydro-9-amino-; Vasicinone(1H-Pyrrоlo[2.1-b]quinazolin-9-one,3-hydroxy-2.3-dihydro) and harmine were isolated from cultivated plant of P. harmala. Four unknown alkaloids were isolated from P. harmala for the first time: 2.2.6.6-Tetramethyl-4-piperidone., Quinoline, 2.3.4-trimethyl-., Pyridine, 2-phenoxy-4- amino- and 4-(3-Propynyloxy)- quinazoline. Their structures were determined by GC-MS.DOI: http://dx.doi.org/10.5564/mjc.v12i0.184 Mongolian Journal of Chemistry Vol.12 2011: 113-116
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9

Sulthana M.T, Chitra K, and Alagarsamy V. "Synthesis of novel 4-oxo-N-(4-oxo-3-substituted-3,4-dihydroquinazolin-2-yl amino)-2-phenylquinazoline-3(4H)-carboxamidines as AntiHIV, antitubercular and antibacterial agents." International Journal of Research in Pharmaceutical Sciences 10, no. 3 (July 19, 2019): 2186–92. http://dx.doi.org/10.26452/ijrps.v10i3.1449.

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A series of novel 4-oxo-N-(4-oxo-3-substituted-3,4-dihydroquinazolin-2-yl amino)-2-phenylquinazoline-3(4H)-carboxamidines are prepared from methyl 4-oxo-2-phenylquinazoline-3(4H)-carbthioimidate & 3-(substituted)-2-hydrazino-quinazoline-4(3H)-ones. The starting material 4-oxo-2-phenylquinazoline-3(4H)-carbthioimidates were prepared from anthranilic acid while the 3-(substituted)-2-hydrazino-quinazolin-4(3H)-one was prepared from a range of 1° amines using multistep preparation. Entire synthesized analogues were screened for their antitubercular, anti-HIV and antibacterial activity. Among the series, N-(3-(4-nitrophenyl)-4-oxo-3,4-dihydroquinazolin-2-yl amino)-4-oxo-2-phenylquinazoline-3(4H)-carboxamidine (BQC7) and N-(3-(4-chlorophenyl)-4-oxo-3,4-dihydroquinazolin-2-yl amino)-4-oxo-2-phenylquinazoline-3(4H)-carboxamidine (BQC9) showed most potent activity against S. epidermidis, S. aureus & B. subtilis with the MIC of 3 µg/mL. The compound BQC7 displayed the antitubercular potency at 12.5 µg/mL and anti-HIV activity at 8.53 µg/mL against HIV1 and HIV2. Thus, these derivatives are useful in the development of novel antitubercular & antiHIV agents. The results obtained from this study confirm that the synthesized and biologically evaluated quinazolines showed promising antimicrobial, antitubercular and anti-HIV activities and are new scaffolds for antimicrobial activity.
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10

Huang, Wei, and Aimin Tan. "4-(4-Amino-2-fluorophenoxy)-7-methoxyquinazolin-6-ol methanol monosolvate." Acta Crystallographica Section E Structure Reports Online 68, no. 4 (March 24, 2012): o1149. http://dx.doi.org/10.1107/s1600536812011725.

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In the title compound, C15H12FN3O3·CH3OH, the dihedral angle between the quinazoline ring system and the benzene ring is 81.18 (9)°. In the crystal, molecules are linked by N—H...O and O—H...N hydrogen bonds, generating [10-1] chains of alternating main molecules and solvent molecules. Weak C—H...O interactions are also observed.
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11

Vashi, R. T., and S. B. Patel. "Synthesis, Characterization and Antifungal Activity of Novel Quinazolin-4-one Derivatives Containing 8-Hydroxyquinazoline Ligand and its Various Metal Complexes." E-Journal of Chemistry 6, s1 (2009): S445—S451. http://dx.doi.org/10.1155/2009/624150.

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Novel ligands containing quinazoline-4-one-8-hydroxyquinoline (QQ) merged moieties were prepared and characterized. For this anthranilic acid and 5-bromoanthranilic acid were converted respectively into 2-chloromethyl–3-(4-methyl phenyl)-3(H)-quinazoline-4-one and 2-chloromethyl–3-(methyl phenyl)-6-bromo-3(H)-quinazoline-4-one. Both these compounds were condensed with 5-amino-8-hydroxyquinoline. The so called resulted compounds were named respectively as 2-[(8-hydroxy-quinolinyl) –5- amino methyl] -3-(4-methylphenyl)- 3(H)- quinazoline -4- one and 2-[(8-hydroxyquinolinyl)-5-aminomethyl] -3(methyl phenyl)-6-bromo-3(H)-quinazoline-4-one. Both the compounds were designated respectively as HL1and HL2ligands. The transition metal (Cu2+, Ni2+, Zn2+, Mn2+and Co2+) complexes of both these ligands were prepared. The ligands and their complexes as case may be were characterized by elemental analysis, spectral studies and number of hydroxyl groups. The stoichiometry of the complexes has been found to be 1:2 (metal: ligand). An octahedral geometry around Co2+, Ni2+and Mn2+, distorted octahedral geometry around Cu2+and tetrahedral geometry of around Zn2+have been proposed. These complexes also been tested for their antifungal activities.
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Yan, He-Ping, Bo Zhou, Gao-Zhang Gou, Ju-Cheng Zhang, Shi-Juan Xu, and Wei Liu. "Synthesis and Characterization of 4-Amino-quinazoline Derivatives." Asian Journal of Chemistry 27, no. 7 (2015): 2460–62. http://dx.doi.org/10.14233/ajchem.2015.17919.

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13

Wang, Xiangshan, Daqing Shi, Shujiang Tu, and Kaibei Yu. "2-Amino-4-phenyl-5,6-dihydrobenzo[h]quinazoline." Acta Crystallographica Section E Structure Reports Online 59, no. 4 (March 7, 2003): o423—o424. http://dx.doi.org/10.1107/s1600536803004616.

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14

Kaliraj, S., R. Jeyalakshmi, M. K. Kathiravan, T. Madhavan, and Arikketh Devi. "Design, Molecular Docking and Biological Evaluation of Fused Thienopyrimidines and Quinazoline." Asian Journal of Chemistry 33, no. 3 (2021): 537–44. http://dx.doi.org/10.14233/ajchem.2021.23062.

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The anticancer activity of the condensed pyrimidine and quinazoline moieties are pronounced with a different pathway. Thienopyrimidine is considered as ring equivalent bioisosteres of quinazolines and present in other heterocyclic compounds including thienopyrimidine. The present investigation focused on the synthesis of thienopyrimidine and quinazoline derivatives for their anticancer activity against the human oral squamous carcinoma-3 (HSC-3) cell line. The synthesized compound confirmed for their structural characteristics from spectral analysis and tested for anti-proliferative activity from MTT assay. The electron-withdrawing group in 4-chloro thienopyrimidines and amino ester derivate/facilitate the inhibition of cancer cells. Further probing by docking studies revealed that the compounds exhibit possible interactions with VEGF, FGFR and c-Met proteins, which are known to have a role in the pathogenesis of oral squamous cell carcinoma. Among the derivatives a moderate activity demonstrated by substituted 4-chloro-5,6,7,8-tetrahydrobenzo[4,5]thieno[2,3-d]-pyrimidine (4a) and ethyl 2-amino-4,5,6,7-tetrahydrobenzo[b]thiophene-3-carboxylate (1a) derivatives. Lack of chirality and the presence of bulky substituents in few of the compounds were found to be the cause for lower potency.
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15

Eweas, Ahmad Farouk, Qasem Mahmoud Aref Abdallah, and Mohamed Fouad Elbadawy. "Synthesis and biological evaluation of some new 2-pyridylquinazoline derivatives." Current Chemistry Letters 10, no. 4 (2021): 459–70. http://dx.doi.org/10.5267/j.ccl.2021.4.005.

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2-pyridyl [3H]-quinazolin-4-one derivatives fused or substituted with different oxygen or nitrogen heterocycle moieties as potential anti-tumor and anti-microbial agents were prepared, characterized and biologically screened. The synthesis process started from 5-bromo-2-[pyridin-4-ylcarbonyl]amino]benzoic acid which was converted to the crucial building block 6-Bromo-2-(pyridin-4-yl)quinazolin-4(3H)-one via two alternative routes. Compound 3 underwent halogenation reaction POCl3 and PCl5 to afford compound 6-Bromo-4-chloro-2-(pyridin-4-yl)quinazoline 4. The novel cyclized products 5a,b-10 were subsequently prepared. Some of the newly synthesized compounds 5a, 5b, 6, 7, 8, 9 and 10 were screened for their antiproliferative and antimicrobial activities against various eukaryotic and prokaryotic cells. Compound 9 showed selective antibacterial activity against Gram-positive bacteria S. aureus (IZ = 26 mm, MIC = 256 µg/ml) and may serve as a good candidate for further developmental studies.
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Shi, Qiu-Zhong, Yong-Nan Cao, Shi-Bing Ma, Guo-Xi Wang, Guang-Fan Han, and Zheng Xing. "Synthesis of Novel Ethyl 1-aryl-3-methyl-8-oxo-1,8-dihydropyrano[2′,3′:4,5] Pyrimido[6,1-b]Quinazoline-2-carboxylate Derivatives." Journal of Chemical Research 40, no. 12 (December 2016): 767–71. http://dx.doi.org/10.3184/174751916x14798109099372.

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In this paper, a new series of ethyl 1-aryl-3-methyl-8-oxo-1,8-dihydropyrano[2′,3′:4,5]pyrimido[6,1-b]quinazoline-2-carboxylate derivatives was synthesised by the cyclisation of methyl anthranilate with ethyl 5-cyano-6-[(ethoxymethylene)amino]-2-methyl-4-aryl-4H-pyran-3-carboxylate derivatives, which were obtained from reaction of triethyl orthoformate with 6-amino-5-cyano-2-methyl-4-aryl-4H- pyran-3-carboxylate derivatives. The title compounds possessed good fluorescence properties. In addition, ethyl 5-cyano-6-[(ethoxymethylene) amino]-2-methyl-4-(p-tolyl)-4H-pyran-3-carboxylate and ethyl 3-methyl-8-oxo-1-(p-tolyl)-1,8-dihydropyrano[2′,3′:4,5]pyrimido[6,1-b] quinazoline-2-carboxylate were further determined by single crystal X-ray diffraction analysis.
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Asquith, Christopher R. M., Tuomo Laitinen, Carrow I. Wells, Graham J. Tizzard, and William J. Zuercher. "New Insights into 4-Anilinoquinazolines as Inhibitors of Cardiac Troponin I–Interacting Kinase (TNNi3K)." Molecules 25, no. 7 (April 7, 2020): 1697. http://dx.doi.org/10.3390/molecules25071697.

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We report the synthesis of several related 4-anilinoquinazolines as inhibitors of cardiac troponin I–interacting kinase (TNNi3K). These close structural analogs of 3-((6,7-dimethoxyquinazolin-4-yl)amino)-4-(dimethylamino)-N-methylbenzenesulfonamide (GSK114) provide new understanding of structure–activity relationships between the 4-anilinoquinazoline scaffold and TNNi3K inhibition. Through a small focused library of inhibitors, we observed that the N-methylbenzenesulfonamide was driving the potency in addition to the more traditional quinazoline hinge-binding motif. We also identified a compound devoid of TNNi3K kinase activity due to the addition of a methyl group in the hinge binding region. This compound could serve as a negative control in the study of TNNi3K biology. Small molecule crystal structures of several quinazolines have been solved, supporting observations made about overall conformation and TNNi3K inhibition.
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Dash, Biswajit, Suvakanta Dash, and Damiki Laloo. "DESIGN AND SYNTHESIS OF 4-SUBSTITUTED QUINAZOLINE DERIVATIVES FOR THEIR ANTICONVULSANT AND CNS DEPRESSANT ACTIVITIES." International Journal of Pharmacy and Pharmaceutical Sciences 9, no. 1 (December 31, 2016): 165. http://dx.doi.org/10.22159/ijpps.2017v9i1.15492.

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<p><strong>Objective: </strong>The present work is designed to synthesise some isomeric new series of Quinazoline-4-one/4-thione derivatives, based on the pharmacophoric model of central nervous system (CNS) activity by structural modifications retaining the essential structural features for the activity and evaluated for their anticonvulsant and CNS depressant properties.</p><p><strong>Methods: </strong>A series of 7-chloro-3-[substituted (amino/phenylamino)]-2-phenyl quinazolin-4 (3H)-one/thione derivatives and 1-(7-chloro-4-oxo/-2-phenylquinazoline-3 (4H-yl)) substituted urea derivatives were prepared. The reaction scheme proceeds through the intermediate 7-chloro-2-phenyl-4H-benzo[d] [1, 3] oxazin-4-one. The structures of the newly synthesised compounds were characterized from infrared (IR), <sup>1</sup>H nuclear magnetic resonance (NMR) and mass spectra (m/z) and elemental analysis. The anti-convulsant and CNS depressant activity were investigated by maximum electroshock (MES) seizure test and porsolt’s behavioural despair test (forced swimming) respectively. The rota-rod test was performed to assess any probable changes in motor coordination induced by the test compounds.</p><p><strong>Results: </strong>The physicochemical and spectroscopic data clearly confirmed the synthesis of quinazoline derivatives with a common skeleton. The synthesised compounds were evaluated for their anticonvulsant and CNS depressant properties. Among them, six compounds <strong>(IIc, </strong>IIg, IIj, IIIc, IIIg, IIIj) exhibited a good activity profile in CNS depressant activity. Five compounds (IIc, IIg, IIj, IIIg, IIIh) showed protection against MES-induced seizures.</p><p><strong>Conclusion: </strong>The Quinazoline derivatives obtained from this research work indicates that the methyl/methoxy group in phenyl ring, amine and thiourea substitution at 3<sup>rd</sup> position of quinazoline derivatives are essential for CNS depressant activity as well as anticonvulsant activity. Compounds IIc, IIg, IIj, IIIc, IIIg, IIIj, and IIIh were found to be a potent compound which may be effective as a potential source for the development of CNS depressant and anti-convulsant drugs with lesser side effects</p>
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Borik, Rita M., and Mohammed A. Hussein. "Synthesis, Molecular Docking, Biological Potentials and Structure Activity Relationship of New Quinazoline and Quinazoline-4-one Derivatives." Asian Journal of Chemistry 33, no. 2 (2021): 423–38. http://dx.doi.org/10.14233/ajchem.2021.23036.

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In this work, a new derivative of ethyl 5-chloro-2-(3-(4-hydroxyphenyl)propanamido)benzoate (1) was synthesized by reacting the amino group of 3-(4-hydroxyphenyl)propanoic acid (0.01 mol) and methyl 2-amino-5-chlorobenzoate in presence of PCl3. Cyclcondensation of 1 with hydrazine hydrate afforded the corresponding 2-(4-hydroxyphenethyl)-3-amino-6-chloroquinazolin-4(3H)-one (2). Also, new Schiff base 3 was prepared via reaction of 2-(4-hydroxyphenethyl)-3-amino-6-chloroquinazolin- 4(3H)-one (2) with 4-hydroxy-3-methoxybenzaldehyde. The synthesized compounds were characterized by elemental analysis, IR, 1H NMR and mass spectral data. Also, the median lethal doses (LD50s) of compounds 1-3 in rats were 1125, 835 and 1785 mg/kg b.w., respectively. IC50 values of compounds (1, 3) as measured by DPPH• method was 136.47 and 73.54 μg/mL, respectively. IC50 values of compounds (1-3) as measured by ABTS•+ radical method was 0.8, 0.92 and 0.08 mg/mL, respectively. Antiulcerogenic activity at dose 1/20 LD50 in albino rats was 47.94, 24.60 and 56.45%, respectively. However, the anti-inflammatory effect at dose 1/20 LD50 of compounds (1-3) induced edema model after 120 min were 74.19, 69.93 and 59.03%, respectively. The synthesized compounds also possess hepatocytes and gastric mucosa protective activity against ibuprofen induced ulceration and LPS-induced liver toxicity, respectively in rats via normalization of oxidative stress biomarkers and inflammatory mediators (Na+/K+-ATPase, ALT, AST, LDH, TNF-α, NO, TBARS, GPx, CAT and SOD). Also, TNF-α, NO, PGE2 and COX-2 were inhibited in peritoneal macrophage cells at a concentration of 100 μg/L. Molecular docking suggested that the most active compounds 1 and 2 can be positioned within the active sites of COX-2 at Arg121 & Tyr356 similarly to ibuprofen (Arg-120, Glu-524 and Tyr-355). The compound 3–COX-2 complex generated by docking, revealed intricate interactions with a COX-2 channel, including hydrogen bonds with key residues Arg121 and phe519. These findings suggest that compounds 1-3 exhibited good antioxidant, antiulcer, anti-inflammatory activity and safe on liver enzymes in rats.
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20

Kopotilova, Alexandra E., Tatyana N. Moshkina, Emiliya V. Nosova, Galina N. Lipunova, Ekaterina S. Starnovskaya, Dmitry S. Kopchuk, Grigory A. Kim, Vasiliy S. Gaviko, Pavel A. Slepukhin, and Valery N. Charushin. "3-Aryl-5-aminobiphenyl Substituted [1,2,4]triazolo[4,3-c]quinazolines: Synthesis and Photophysical Properties." Molecules 28, no. 4 (February 17, 2023): 1937. http://dx.doi.org/10.3390/molecules28041937.

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Amino-[1,1′]-biphenyl-containing 3-aryl-[1,2,4]triazolo[4,3-c]quinazoline derivatives with fluorescent properties have been designed and synthesized. The type of annelation of the triazole ring to the pyrimidine one has been unambiguously confirmed by means of an X-ray diffraction (XRD) method; the molecules are non-planar, and the aryl substituents form the pincer-like conformation. The UV/Vis and photoluminescent properties of target compounds were investigated in two solvents of different polarities and in a solid state. The samples emit a broad range of wavelengths and display fluorescent quantum yields of up to 94% in toluene solutions. 5-(4’-Diphenylamino-[1,1′]-biphenyl-4-yl)-3-(4-(trifluoromethyl)phenyl)-[1,2,4]triazolo[4,3-c]quinazoline exhibits the strongest emission in toluene and a solid state. Additionally, the solvatochromic properties were studied for the substituted [1,2,4]triazolo[4,3-c]quinazolines. Moreover, the changes in absorption and emission spectra have been demonstrated upon the addition of water to MeCN solutions, which confirms aggregate formation, and some samples were found to exhibit aggregation-induced emission enhancement. Further, the ability of triazoloquinazolines to detect trifluoroacetic acid has been analyzed; the presence of TFA induces changes in both absorption and emission spectra, and acidochromic behavvior was observed for some triazoloquinazoline compounds. Finally, electronic-structure calculations with the use of quantum-chemistry methods were performed for synthesized compounds.
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21

El-Shanawany, Mohamed A., Hanaa M. Sayed, Sabrin R. M. Ibrahim, and Marwa A. A. Fayed. "New Nitrogenous Compounds from Anisotes trisulcus." Zeitschrift für Naturforschung C 69, no. 5-6 (June 1, 2014): 209–18. http://dx.doi.org/10.5560/znc.2013-0116.

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Re-investigation of the methanolic extract of Anisotes trisulcus (Forssk.) Nees aerial parts led to the isolation of two new tricyclic quinazoline alkaloids, 8-amino-7,8,9,11-tetrahydro-6H-pyrido[2,1-b]- quinazoline-2,6-diol (4) and 8-amino-3,6-dihydroxy-7,8,9-trihydro-6H-pyrido[2,1-b]quinazoline- 11-one (5), and two quaternary ammonium compounds, (dimethylamino)-N-(hydroxymethyl)-N,Ndimethyl methanaminium chloride (6) and N-[(carboxyamino)methyl]-N,N-dimethyl ethanaminium chloride (7), together with three known compounds, peganine (1), vasicinone (2), and anisotine (3). The structures of these compounds were established on the basis of physical, chemical, and spectral data (UV, IR, MS, 1D and 2D NMR), as well as by comparison with authentic samples. GC-MS analysis of the fatty acid methyl esters and unsaponifiable matter revealed the presence of 46 fatty acids, 53 hydrocarbons, and 18 sterols. The different extracts were evaluated for their antihyperglycaemic activities. The MeOH, n-hexane, and EtOAc extracts exhibited a significant hypoglycaemic effect
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22

Moustafa, Moustafa Sherief, Saleh Mohammed Al-Mousawi, Maghraby Ali Selim, Ahmed Mohamed Mosallam, and Mohamed Hilmy Elnagdi. "Organobase-catalyzed three-component reactions for the synthesis of 4H-2-aminopyrans, condensed pyrans and polysubstituted benzenes." Beilstein Journal of Organic Chemistry 10 (January 14, 2014): 141–49. http://dx.doi.org/10.3762/bjoc.10.11.

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Novel routes for the preparation of 2-amino-4H-pyran-3-carbonitrile 9, amino-arylbenzoic acid ester derivatives 13a,b, 2-aminotetrahydro-4H-chromene-3-carbonitrile 18, 3-amino-4-cyanotetrahydronaphthalene-2-carboxylic acid ester 26 and 4-amino-3,5-dicyanophthalic acid ester derivatives 37a–c were developed. The synthetic methods utilize one-pot reactions of acetylene carboxylic acid esters, α,β-unsaturated nitriles and/or active methylenenitriles in the presence of L-proline or DABCO. Plausible mechanisms are suggested for the formation of the products. Finally, these compounds were used for the efficient synthesis of 6-amino-5-cyanonicotinic acid ester derivatives 31a,b, ethyl 4-amino-5H-pyrano[2,3-d]pyrimidine-6-carboxylates 33a,b, 4-amino-6H-pyrrolo[3,4-g]quinazoline-9-carbonitrile 39, and 1,7-diamino-6-(N'-hydroxycarbamimidoyl)-3-oxo-5-phenyl-3H-isoindole-4-carboxylate (40).
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23

Sunil Kumar, A., Jyothi Kudva, Manu Lahtinen, Anssi Peuronen, Rajitha Sadashiva, and Damodara Naral. "Synthesis, characterization, crystal structures and biological screening of 4-amino quinazoline sulfonamide derivatives." Journal of Molecular Structure 1190 (August 2019): 29–36. http://dx.doi.org/10.1016/j.molstruc.2019.04.050.

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24

Geffken, Detlef, and Maria Anna Köllner. "Cyclisierung von N′,N′-disubstituierten Anthranilsäurehydraziden mit 1,1′-Oxalyldiimidazol zu 4-Amino-2,3,4,5-tetrahydro-1H-1,4-benzodiaz- epin-2,3,5-trionen / Cyclization of N’,N’-Disubstituted Anthranilic Hydrazides with 1,1’-Oxalyldiimidazole to 4-Amino-2,3,4,5-tetrahydro-1H-1,4-benzodiazepin-2,3,5-triones." Zeitschrift für Naturforschung B 60, no. 11 (November 1, 2005): 1207–11. http://dx.doi.org/10.1515/znb-2005-1115.

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N’,N’-Disubstituted (2-phenylamino)-, (2-methylamino)- and (2-benzylamino)benzohydrazides (1) are cyclized by in situ prepared 1,1’-oxalyldiimidazole to give 3-amino-2,3,4,5-tetrahydro-1H- 1,4-benzodiazepine-2,3,5-triones 2 as the major product. Depending on the substituents of 1 competitive formation of quinazoline-2,4-diones 3 and 1,3,4-oxadiazoline-2-one 4 is observed. The formation of heterocycles 2, 3, 4 is rationalized via a common primary intermediate 1A.
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25

Chernyshev, Vladimir V., Denis Machon, Andrew N. Fitch, Sergei A. Zaitsev, Alexandr V. Yatsenko, Alexandr N. Shmakov, and Hans-Peter Weber. "Protonation site and hydrogen bonding in anhydrous and hydrated crystalline forms of doxazosin mesylate from powder data." Acta Crystallographica Section B Structural Science 59, no. 6 (November 25, 2003): 787–93. http://dx.doi.org/10.1107/s0108768103022729.

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The three-dimensional solid-state structures of two modifications of doxazosin mesylate C23H26N5O_5^+·CH3SO_3^-, 4-amino-2-[4-[(2,3-dihydro-1,4-benzodioxin-2-yl)carbonyl]piperazin-1-yl]-6,7-dimethoxyquinazoline methanesulfonate, a commonly used antihypertensive agent, have been determined by synchrotron X-ray powder diffraction. An anhydrous form (A) and a dihydrate form (d G) crystallize in monoclinic space groups. In both forms the doxazosin molecule is protonated at the N1 atom of the quinazoline bicycle. The N1 atom, and the amino H atoms and O atoms of the mesylate moieties are involved in three-dimensional hydrogen-bonding networks, while solvent water molecules and carboxamide O atoms are also incorporated in a hydrogen-bonding network in d G.
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26

SHAFI, S. SYED, P. SUBASHINI, S. GAJALAKSHMI, and V. VIJAYA KUMAR. "An Efficient Suitable Synthesis for Pyrazole, Pyrimidine Derivatives and Biological Evaluation." Asian Journal of Chemistry 33, no. 4 (March 20, 2021): 734–40. http://dx.doi.org/10.14233/ajchem.2021.23095.

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Novel quinazoline derivatives were synthesized by reacting isatoic anhydride and 4-amino acetanilide to synthesize N-(4-(2,4-dioxo-1,2- dihydroquinazolin-3(4H)-yl)phenyl)acetamide which in turn reacted with substituted aromatic aldehydes to synthesize novel chalcones. The chalcones were allowed to react with hydrazine hydrochloride and guanidine to form pyrazoline and pyrimidine derivatives, respectively. The newly synthesized compounds were characterized by IR, NMR (1H, 13C), mass and elemental analysis. All the newly synthesized derivatives were screened for in vitro antimicrobial and antioxidant activities to evaluate their biological potency.
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27

Roudbaraki, Seyyed Jalal, Sadaf Janghorban, and Majid Ghashang. "Green Chemistry Preparation of thiochromeno[4,3-b]pyran and benzo[h]thiazolo[2,3-b]quinazoline Derivatives using HSBM Technique over ZnAl2O4 Nano-Powders." Combinatorial Chemistry & High Throughput Screening 22, no. 6 (September 5, 2019): 421–27. http://dx.doi.org/10.2174/1386207322666190617164617.

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Aim and Objective: The aim of this paper is to introduce HSBM as a green and environmentally friendly technique for the synthesis of thiochromeno[4,3-b]pyran and benzo[h]thiazolo[2,3-b]quinazoline derivatives over ZnAl2O4 nanopowders as an efficient catalyst. Materials and Methods: ZnAl2O4 nanopowders were synthesized via a co-precipitation of Zn(NO3)2 and Al(NO3)3 salts and were characterized by XRD, FE-SEM, TEM and DLS techniques. The as-prepared ZnAl2O4 nano-powders have been used as a catalyst on the synthesis of pyran nucleus using high-speed ball milling (HSBM) technique. The structure of products was confirmed with NMR analysis. Results: ZnAl2O4 exhibits a cubic crystal structure (Space group: Fd-3m) with the average crystallite size of 41 nm. The average particle size of ZnAl2O4 nano-powders determined by DLS technique is 55 nm. The catalytic activity of nano-powders was examined on the synthesis of 2- amino-4,5-dihydro-4-arylthiochromeno[4,3-b]pyran-3-carbonitriles, (8Z)-2-amino-8-arylidene-4,5, 7,8-tetrahydro-4-arylthiopyrano[4,3-b]pyran-3-carbonitriles, 4-aryl-3,4,5,6-tetrahydrobenzo[h]quinazoline- 2(1H)-thiones and 4-aryl-1,3,4,5-tetrahydro-2H-thiochromeno[4,3-d]pyrimidine-2-thione derivatives. All products were obtained in high yields with short reaction times. Conclusion: ZnAl2O4 nanopowders were prepared via a cost-effective co-precipitation method and showed good potential for the synthesis of 4H-pyran analogous in good yields. The salient advantages of HSBM technique include environmentally friendly with reduced solvents, is a simple technique and has low energy costs.
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28

Marinho, Elina, and M. Fernanda Proença. "Acid catalyzed synthesis of 2-(2-aminophenyl)quinazoline-4-amine and reaction with aromatic aldehydes." RSC Advances 6, no. 8 (2016): 6138–43. http://dx.doi.org/10.1039/c5ra19785f.

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The hydrochloride salt of 2-(2-aminophenyl)quinazoline-4-amine, prepared from a quinazolino[3,4-a]quinazoline, was reacted with aromatic aldehydes under conventional heating or microwave irradiation, leading to tetracyclic dihydroquinazolines.
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29

Keruckiene, Rasa, Simona Vekteryte, Ervinas Urbonas, Matas Guzauskas, Eigirdas Skuodis, Dmytro Volyniuk, and Juozas V. Grazulevicius. "Synthesis and properties of quinazoline-based versatile exciplex-forming compounds." Beilstein Journal of Organic Chemistry 16 (May 28, 2020): 1142–53. http://dx.doi.org/10.3762/bjoc.16.101.

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Three compounds, bearing a quinazoline unit as the acceptor core and carbazole, dimethyldihydroacridine, or phenothiazine donor moieties, were designed and synthesized in two steps including a facile copper-catalyzed cyclization and a nucleophilic aromatic substitution reaction. The photophysical properties of the compounds, based on theoretical calculations and experimental measurements, as well as the electrochemical and thermal properties, are discussed. The synthesized compounds form glasses with glass-transition temperatures ranging from 116 °C to 123 °C. The ionization potentials estimated by cyclic voltammetry of the derivatives were in the range of 5.22–5.87 eV. The 3,6-di-tert-butylcarbazole-substituted quinazoline-based compound forms a sky-blue emitting exciplex in solid mixture with the acceptor 2,4,6-tris[3-(diphenylphosphinyl)phenyl]-1,3,5-triazine as well as an orange emitting exciplex with the donor 4,4′,4″-tris[3-methylphenyl(phenyl)amino]triphenylamine. A white OLED based on these versatile exciplex systems with a relatively high maximum brightness of 3030 cd/m2 and an external quantum efficiency of 0.5% was fabricated.
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30

Kalniņa, A., Ē. Bizdēna, G. Kiselovs, A. Mishnev, and M. Turks. "Structural Proof of Tetrazolo[1,5-a]quinazoline Derivatives and their Application in the Synthesis of 4-Amino-2-(1,2,3-triazol-1-yl)quinazolines*." Chemistry of Heterocyclic Compounds 49, no. 11 (January 28, 2014): 1667–73. http://dx.doi.org/10.1007/s10593-014-1418-2.

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31

Sunil Kumar, A., Jyothi Kudva, S. Madan Kumar, U. Vishwanatha, Vasantha Kumar, and Damodara Naral. "Synthesis, characterization, crystal structure, Hirshfeld interaction and bio-evaluation studies of 4-amino quinazoline sulfonamide derivatives." Journal of Molecular Structure 1167 (September 2018): 142–53. http://dx.doi.org/10.1016/j.molstruc.2018.04.055.

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32

Cho, Nam-Chul, Ji Hyoun Cha, Hyojin Kim, Jinsook Kwak, Dohee Kim, Seung-Hwan Seo, Ji-Sun Shin, et al. "Discovery of 2-aryloxy-4-amino-quinazoline derivatives as novel protease-activated receptor 2 (PAR2) antagonists." Bioorganic & Medicinal Chemistry 23, no. 24 (December 2015): 7717–27. http://dx.doi.org/10.1016/j.bmc.2015.11.016.

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33

Elsherbeny, Mohamed H., Usama M. Ammar, Magda H. Abdellattif, Mohammed A. S. Abourehab, Ahmed Abdeen, Samah F. Ibrahim, Doaa Abdelrahaman, Wessam Mady, Eun Joo Roh, and Ahmed Elkamhawy. "2-(3-Bromophenyl)-8-fluoroquinazoline-4-carboxylic Acid as a Novel and Selective Aurora A Kinase Inhibitory Lead with Apoptosis Properties: Design, Synthesis, In Vitro and In Silico Biological Evaluation." Life 12, no. 6 (June 10, 2022): 876. http://dx.doi.org/10.3390/life12060876.

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New quinazoline derivatives were designed based on the structural modification of the reported inhibitors to enhance their selectivity toward Aurora A. The synthesized compounds were tested over Aurora A, and a cytotoxicity assay was performed over NCI cell lines to select the best candidate for further evaluation. Compound 6e (2-(3-bromophenyl)-8-fluoroquinazoline-4-carboxylic acid) was the most potent compound among the tested derivatives. A Kinase panel assay was conducted for compound 6e over 14 kinases to evaluate its selectivity profile. Further cell cycle and apoptosis analysis were evaluated for compound 6e over the MCF-7 cell line at its IC50 of 168.78 µM. It arrested the cell cycle at the G1 phase and induced apoptosis. Molecular docking was performed to explore the possible binding mode of compound 6e into the active site. It showed significant binding into the main pocket in addition to potential binding interactions with the key amino acid residues. Accordingly, compound 6e can be considered a potential lead for further structural and molecular optimization of the quinazoline-based carboxylic acid scaffold for Aurora A kinase selective inhibition with apoptosis properties.
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34

Zieliński, Wojciech, and Agnieszka Kudelko. "A study concerning the synthesis, basicity and hydrolysis of 4-amino-2-(N,N-diethylamino)quinazoline derivatives." Journal of Heterocyclic Chemistry 39, no. 6 (November 2002): 1289–92. http://dx.doi.org/10.1002/jhet.5570390627.

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35

Osarumwense, P. O., M. O. Edema, and C. O. Usifoh. "Synthesis And Anagesic activities of Quinazolin-4(3H)-One, 2-Methyl-4(3H)-Quinazolinone and 2–Phenyl-4(3H)-quinazolin-4(3H)–one." Journal of Drug Delivery and Therapeutics 10, no. 4-s (August 15, 2020): 87–91. http://dx.doi.org/10.22270/jddt.v10i4-s.4209.

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Background: Objective: The current study is aimed at the synthesis of these quinazolinone derivatives quinazolin-4(3H)-One, 2-Methyl-4(3H)-quinazolinone and 2–Phenyl-4(3H)-quinazolin-4(3H)–one and evaluate them for their analgesic activity. Method: The condensation of 2-amino-methyl-4-methoxybenzoate with acetic anhydride yielded the cyclic compound 2-methyl-4, 5-disubstituted-1, 3-benzo-oxazine-4-one which further produce a novel 2,3-disubstituted quinazolin-4 ones via the reaction with hydrazine hydrate The quinazolinone derivatives quinazolin-4(3H)-One, 2-Methyl-4(3H)-quinazolinone and 2–Phenyl-4(3H)-quinazolin-4(3H)–one were evaluated pharmacologically for their in vivo analgesic activities by acetic acid induced writhing in mice. The compounds synthesized were unequivocally confirmed by means of Infrared, Nuclear Magnetic Resonance (1H and 13C), Gas Chromatography Mass Spectrophotometer and Elemental analysis.The synthesized compounds were screened for their analgesic activity.Compounds 1,2 and 3 showed significant analgesic activity. Discussion: Compound 1 was characterized by the absence of methyl group and the presence of methyl group for compound 2. The test investigated compounds exhibited significant analgesic activity when compared with the control test sample. The compounds synthesized exhibited promising analgesic activities against . Conclusion: The compounds have high analgesic activity. Compound 3 has a higher activity compared to Compound 2 and compound 2 has a higher analgesic activity compared to compound 1. Compound 3 has a higher analgesic activity compared to the standard drugs Aspirin and Indomethacin. Keywords: quinazolin-4(3H)-One, 2-Methyl-4(3H)-quinazolinone and 2–Phenyl-4(3H)-quinazolin-4(3H)–one quinazolin-4(3H)-one, analgesic activity.
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36

Behjet, Shaimaa A., and Zahraa F. Khudair. "Synthesis and Characterization of Some New Heterocyclic Derivatives and Studying of their Biological Activity (Anti-Bacteria)." INTERNATIONAL JOURNAL OF PHARMACEUTICAL QUALITY ASSURANCE 11, no. 01 (March 25, 2020): 38–44. http://dx.doi.org/10.25258/ijpqa.11.1.6.

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Introduction: In this work synthesis, many kinds of heterocyclic derivatives by many steps, the first we preparation 1-(4-((1H-imidazol_2-yl-) diazenyl) phenyl) ethan-1_one. (1) by coupling of diazonium salt of p-amino acetophenone with imidazole in alkaline alcoholic media, the second step include react (1) with 2_amino_6_methylpyrimidin _4_ol in acid medium to get Schiff base derivatives(2)the last step include react(2) with (sodium azide, thioglycolic acid, glycine, alanine, Tryptophan, (2 aminobenzoic acid), (2-mercaptobenzoic acid) to give (tetrazole(3), thiazolidine(4), imidazolidine(5-7), Thiazinie(8), Quinazoline (9) derivatives, respectively. All these derivatives Characterization by FTIR, 1HNMR, 13C-NMR, After that we studied the biological activity for all derivatives for all derivatives studied the anticancer for (2).
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37

Kalnina, A., E. Bizdena, G. Kiselovs, A. Mishnev, and M. Turks. "ChemInform Abstract: Structural Proof of Tetrazolo[1,5-a]quinazoline Derivatives and Their Application in the Synthesis of 4-Amino-2-(1,2,3-triazol-1-yl)quinazolines." ChemInform 45, no. 24 (June 2, 2014): no. http://dx.doi.org/10.1002/chin.201424179.

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38

Popov, L. D., S. A. Borodkin, V. V. Tkachev, Yu P. Tupolova, A. S. Burlov, G. V. Shilov, and A. N. Utenyshev. "Crystal structure of copper(II) 2-methyl-3-{[3-methyl-5-oxo-1-phenylpyrazole-4-ylidene-methyl]amino}-quinazoline-4-onate." Journal of Structural Chemistry 58, no. 2 (March 2017): 358–61. http://dx.doi.org/10.1134/s0022476617020196.

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39

Zheng, Qing, Yang Zhang, Yong Dai, and Xiangyun Han. "Vibrational Spectroscopic Investigation and Theoretical Calculations of (E)-3-Phenyl-N-[4-(Phenyl-Amino) Quinazoline-7-yl] Acrylamide." Spectroscopy Letters 45, no. 7 (October 1, 2012): 530–40. http://dx.doi.org/10.1080/00387010.2011.650812.

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40

Mphahlele, Malose, Mmakwena Mmonwa, Abimbola Aro, Lyndy McGaw, and Yee Choong. "Synthesis, Biological Evaluation and Molecular Docking of Novel Indole-Aminoquinazoline Hybrids for Anticancer Properties." International Journal of Molecular Sciences 19, no. 8 (July 31, 2018): 2232. http://dx.doi.org/10.3390/ijms19082232.

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A series of indole-aminoquinazolines was prepared via amination of the 2-aryl-4-chloroquinazolines with the 7-amino-2-aryl-5-bromoindoles. It was then evaluated for cytotoxicity in vitro against human lung cancer (A549), epithelial colorectal adenocarcinoma (Caco-2), hepatocellular carcinoma (C3A), breast adenocarcinoma (MCF-7), and cervical cancer (HeLa) cells. A combination on the quinazoline and indole moieties of a 2-phenyl and 2-(4-fluorophenyl) rings in compound 4b; 2-(4-fluorophenyl) and 3-chlorophenyl rings in compound 4f; or the two 2-(4-fluorophenyl) rings in compound 4g, resulted in significant and moderate activity against the Caco-2 and C3A cell lines. The indole-aminoquinazoline hybrids compounds 4f and 4g induced apoptosis in Caco-2 and C3A cells, and were also found to exhibit moderate (IC50 = 52.5 nM) and significant (IC50 = 40.7 nM) inhibitory activity towards epidermal growth factor receptor (EGFR) against gefitinib (IC50 = 38.9 nM). Molecular docking suggests that 4a–h could bind to the ATP region of EGFR like erlotinib.
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41

Makrypidi, Konstantina, Christos Kiritsis, Ioanna Roupa, Sotiria Triantopoulou, Antonio Shegani, Maria Paravatou-Petsotas, Aristeidis Chiotellis, Maria Pelecanou, Minas Papadopoulos, and Ioannis Pirmettis. "Evaluation of Rhenium and Technetium-99m Complexes Bearing Quinazoline Derivatives as Potential EGFR Agents." Molecules 28, no. 4 (February 14, 2023): 1786. http://dx.doi.org/10.3390/molecules28041786.

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Τhe Epidermal Growth Factor Receptor tyrosine kinase inhibitor (EGFR-TKI) 6-amino-4-[(3-bromophenyl) amino]quinazoline was derivatized with 6-bromohexanoyl-chloride and coupled with the tridentate chelating agents N-(2-pyridylmethyl) aminoethyl acetic acid (PAMA) and L(+)-cysteine bearing the donor atom set NNO and SNO, respectively. The rhenium precursors ReBr(CO)5 and fac-[NEt4]2[ReBr3(CO)3] were used for the preparation of the Re complexes fac-[Re(NNO)(CO)3] (5a) and fac-[Re(SNO)(CO)3] (7a) which were characterized by NMR and IR spectroscopies. Subsequently, the new potential EGFR inhibitors were labeled with the fac-[99mTc(CO)3]+ core in high yield and radiochemical purity (>90%) by ligand exchange reaction using the fac-[99mTc][Tc(OH2)3(CO)3]+ precursor. The radiolabeled complexes were characterized by comparative HPLC analysis with the analogous rhenium (Re) complexes as references. In vitro studies in the A431 cell lines showed that both ligands and Re complexes inhibit A431 cell growth. Complex 5a demonstrated the highest potency (IC50 = 8.85 ± 2.62 μM) and was further assessed for its capacity to inhibit EGFR autophosphorylation, presenting an IC50 value of 26.11 nM. Biodistribution studies of the 99mTc complexes in healthy mice showed high in vivo stability for both complexes and fast blood and soft tissue clearance with excretion occurring via the hepatobiliary system.
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42

Rueeger, Heinrich, Pascal Rigollier, Yasuchika Yamaguchi, Tibur Schmidlin, Walter Schilling, Leoluca Criscione, Steven Whitebread, et al. "Design, synthesis and SAR of a series of 2-substituted 4-amino-quinazoline neuropeptide Y Y 5 receptor antagonists." Bioorganic & Medicinal Chemistry Letters 10, no. 11 (June 2000): 1175–79. http://dx.doi.org/10.1016/s0960-894x(00)00177-3.

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43

Santagati, Andrea, Maria Modica, Luigi Monsù Scolaro, and Maria Santagati. "New Synthetic Approaches to Fused Heterocyclo-quinazolines." Journal of Chemical Research 23, no. 2 (February 1999): 86–87. http://dx.doi.org/10.1177/174751989902300210.

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Fused heterocyclo-quinazolines have been prepared from the versatile and easily obtained intermediate 3-amino-2,3-dihydro-2-thioxo-4(1 H)-quinazolinone 2; their structural elucidation is also reported.
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44

Reddy, Gajjala Raghavendra, Chinta Raveendra Reddy, Gopireddy Venkata Subba Reddy, Pasupuleti Visweswara Rao, Meenakshisundaram Swaminathan, Balam Satheeh Krishna, and Cirandur Suresh Reddy. "Synthesis of New 4-Chloro-6-Methylpyrimidin-2-yl-Aminophosphonates as Potential DU145 and A549 Cancer Cell Inhibitors." Letters in Drug Design & Discovery 17, no. 4 (April 25, 2020): 396–410. http://dx.doi.org/10.2174/1570180816666190329223207.

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: A series of new α-aminophosphonates containing potential anticancer active 4-chloro-6- methylpyrimidin-2-amino pharmacophore were synthesized. Background: α-Aminophosphonates are of growing interest to the researchers due to their biological activities. Besides aminophosphoryl functionality, which is responsible for the vital activity, incorporation of a captivating pharmacophore on it will definitely enrich its activity. Objective: Erstwhile many of the reported α-aminophosphonates impregnated with bioactive heterocycles like quinazoline, chromene, pyrazole, furan and thiophene were used as anticancer drugs, and we are intended to enhance the anticancer potentiality of α-aminophosphonates by substituting a new 4-chloro-6-methylpyrimidin-2-yl group into its structure, specifically on nitrogen atom. Methods: Title compounds were synthesized by Kabachnik-Fields reaction by using sulfated Titania, a solid acid catalyst that is encompassed with high density of Lewis acidic reaction sites. The series of synthesized compounds were screened for in vitro anti-cancer activity and their ADMET, QSAR and drug properties studied. Results: Structures of all the title compounds synthesized in high yields were confirmed by spectral & elemental analyses. Their anti-cancer screening studies on various cell lines and evaluation of other properties revealed their potentiality towards the inhibition of growth of DU145 & A549 cell lines. Conclusion: The substitution of 4-chloro-6-methylpyrimidin-2-amino moiety on to the amino functionality of the α-aminophosphonates is a critical task invariably due to the substitutions that are located on α-carbon. As such, this substitution had increased the scope for growth inhibition of DU145 and A549 cancer cells.
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45

Awad, Mohamed K., Mahmoud F. Abdel-Aal, Faten M. Atlam, and Hend A. Hekal. "Synthesis of New α-Amino Phosphonates Containing 3-Amino-4(3H) Quinazolinone Moiety as Anticancer and Antimicrobial Agents: DFT, NBO, and Vibrational Studies." Current Organic Synthesis 15, no. 2 (April 24, 2018): 286–96. http://dx.doi.org/10.2174/1570179414666170703141629.

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Aim and Objective: Synthesis of new .-aminophosphonates containing quinazoline moiety through Kabachnik-Fields reaction in the presence of copper triflate catalyst [32], followed by studying their antimicrobial activities and in vitro anticancer activities against liver carcinoma cell line (HepG2) with the hope that new anticancer agents could be developed. Also, the quantum chemical calculations are performed using density functional theory (DFT) to study the effect of the changes of molecular and electronic structures on the biological activity of the investigated compounds. Materials and Method: The structures of the synthesized compounds are confirmed by FT-IR, 1H NMR, 13C NMR, 31P NMR and MS spectral data. The synthesized compounds show significant antimicrobial and also remarkable cytotoxicity anticancer activities against liver carcinoma cell line (HepG2). Density functional theory (DFT) was performed to study the effect of the molecular and electronic structure changes on the biological activity. Results: It was found that the electronic structure of the substituents affects on the reaction yield. The electron withdrawing substituent, NO2 group 3b, on the aromatic aldehydes gave a good yield more than the electron donating substituent, OH group 3c. The electron deficient on the carbon atom of the aldehydic group may increase the interaction of the Lewis acid (Cu(OTf)2) and the Lewis base (imine nitrogen), and accordingly, facilitate the formation of imine easily, which is attacked by the nucleophilic phosphite species to give the α- aminophosphonates. Conclusion: The newly synthesized compounds exhibit a remarkable inhibition of the growth of Grampositive, Gram-negative bacteria and fungi at low concentrations. The cytotoxicity of the synthesized compounds showed a significant cytotoxicity against the liver cancer cell line (HepG 2). Also, it was shown from the quantum chemical calculations that the electron-withdrawing substituent increases the biological activity of the α-aminophosphonates more than the electron donating group which was in a good agreement with the experimental results. Also, a good agreement between the experimental FT-IR and the calculated one was found.
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46

Panneerselvam, Theivendren, Palanirajan Vijayaraj Kumar, Chinnasamy Rajaram Prakash, and Sundararajan Raja. "Synthesis and anticonvulsant activity of 6,7,8,9-tetra hydro-5H-5-(2′-hydroxy phenyl)-2-(4′-substituted benzylidine)-3-(4-nitrophenyl amino) thiazolo quinazoline derivatives." Toxicological & Environmental Chemistry 93, no. 4 (April 2011): 643–55. http://dx.doi.org/10.1080/02772248.2011.556636.

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47

Osarumwense, Peter O. "Analgesic activity of newly synthesized 7-chloro–2–methyl-4H–benzo[d] [1,3]–oxazin–4–one and 3–amino-7-chloro-2–methyl-quinazolin-4(3H)–one." Ovidius University Annals of Chemistry 29, no. 1 (June 28, 2018): 25–28. http://dx.doi.org/10.2478/auoc-2018-0003.

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Abstract The current study is aimed at the analgesic evaluation of quinazolinone derivatives. The quinazolinone derivatives 7-chloro-2-methyl-4H-benzo[d][1,3]-oxazin-4-one and 3-amino-7-chloro-2-methyl-quinazolin-4(3H)-one were evaluated pharmacologically for their in vivo analgesic activities by acetic acid induced writhing in mice. The compounds exhibited significant analgesic activity in the range of 74.67 - 83.80% in comparison to control.
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48

Nguyen, Thi Ngoc, Thi Huong Tran, Nguyet Suong Huyen Dao, Van Giang Nguyen, Dinh Luyen Nguyen, Nguyen Trieu Trinh, and Van Hai Nguyen. "Synthesis and Spectral Characterization of 4,7-Dichloro-6-nitroquinazoline." Molbank 2020, no. 2 (May 11, 2020): M1134. http://dx.doi.org/10.3390/m1134.

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Afatinib is a 4-anilinoquinazoline tyrosine kinase inhibitor (TKI) in the form of a dimaleate salt which is indicated for the treatment of locally advanced or metastatic non-small cell lung cancer (NSCLC). The most scalable route for the synthesis of this drug was reported in two Boehringer Ingelheim patents, in which the title compound, 4,7-dichloro-6-nitroquinazoline (IV), is an important intermediate. Compound IV is also present in a number of synthetic pathways for various 4,7-disubstituted quinazoline derivatives displaying high therapeutic potential. However, no detailed characterization of this popular compound has been reported, possibly due to its high instability. In this paper, IV was prepared in an overall yield of 56.1% by a 3-step process (condensation, nitration, and chlorination) from 2-amino-4-chlorobenzoic acid (I). The target compound has been for the first time fully characterized by melting point, mass-spectrometry, FT-IR, 1H-NMR and 13C-NMR spectroscopies.
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49

Singh, Shiv Dev, Arvind Kumar, Firoz Babar, Neetu Sachan, and Arun Kumar Sharma. "Synthesis of Novel 3(N,N-dialkylamino)alkyl/phenyl Substituted Thieno [2,3-d]pyrimidinones as H1-Anti-Histaminic and Antimicrobial Agents." Current Bioactive Compounds 15, no. 1 (February 6, 2019): 63–70. http://dx.doi.org/10.2174/1573407214666180226130957.

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Background: Thienopyrimidines are the bioisoster of quinazoline and unlike quinazoline exist in three isomeric forms corresponding to the three possible types annulation of thiophene to the pyrimidine ring viz thieno[2,3-d] pyrimidine, thieno[3,2-d] pyrimidine and thieno[3,4-d]pyrimidine. Heterocyclic containing the thienopyrimidinone moiety exhibits various pronounced activities such as anti-hypertensive, analgesic and anti-inflammatory, antiviral, platelet aggregation inhibitory, antiprotozoal bronchodilatory, phosphodiesterase inhibitory, antihistaminic, antipsychotic and antimicrobial activity. Objective: Synthesis of novel 3(N,N-dialkylamino)alkyl/phenyl substituted thieno[2,3-d]pyrimidinones as H1-anti-histaminic and antimicrobial agents. Methods: A series of 3-[(N,N-dialkylamino)alkyl/phenyl]-2-(1H)thioxo-5,6,7,8-tetrahydrobenzo(b) thieno(2,3-d)pyrimidine-4(3H)-ones[4a-d], their oxo analogous [5a-d] and 3-[(N,N-dialkylamino)alkyl]- 2-chlorophenyl-5,6,7,8-tetrahydrobenzo(b)thieno(2,3-d)pyrimidine- 4 (3H)-ones[6a-d]derivative were synthesized from 2-amino-4,5,6,7-tetrahydrobenzo(b)thiophene-3-carboxylic acid by nucleophilic substitution of different N,N-dialkyl alkylene/phenylene diamines on activated 3-acylchloride moiety followed by cyclocondensation with carbon disulfide and ethanolic potassium hydroxide to get [4a-d] and in second reaction by condensation with 4-chlorobenzoyl chloride to get [6a-d] by single pot novel innovative route. The oxo analogous [5a-d] were prepared by treating derivatives [4a-d] with potassium permagnate in ethanolic KOH. The synthesized compound were evaluated for H1-antihistaminic and antimicrobial activities. Results: All synthesized compounds exhibited significant H1-antihistaminic activity by in vitro and in vivo screening methods and data were verified analytically and statistically. The compound 4a, 4b, 5a and 5b showed significant H1-antihistaminiic activity than the reference standard chlorpheniramine maleate. The compound 6d, 6c, 5c and 4c exhibited significant antimicrobial activity.
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50

Santos-Cruz, Luis Felipe, Bertha Guadalupe Ramírez-Cruz, Miguel García-Salomé, Zaira Yuriria Olvera-Romero, Francisco Hernández-Luis, Luis Barbo Hernández-Portilla, Ángel Durán-Díaz, et al. "Genotoxicity assessment of four novel quinazoline-derived trypanocidal agents in the Drosophila wing somatic mutation and recombination test." Mutagenesis 35, no. 4 (December 3, 2019): 299–310. http://dx.doi.org/10.1093/mutage/gez042.

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Abstract Chagas disease, caused by the protozoan Trypanosoma cruzi, has increased in the world due to migration, travelling and climate change; at present, the principal problem is that common trypanocidal agents have resulted in toxic or inconvenient side effects. We tested for genotoxicity in the standard (ST) and high bioactivation (HB) crosses of Drosophila wing somatic mutation and recombination test, four novel trypanocidal agents derived from 2, 4, 6-triaminquinazoline (TAQ): 2,4-diamino-6 nitro-1,3 diazonaftalene (S-1QN2-1), 2,4-diacetamino-6-amino 1,3 diazonaftalene (D-1), N6-(4,methoxybenzyl)quinazoline-2,4,6-triamine (GHPM) and N6-[4-(trifluoromethoxy)benzyl]quinazoline-2,4,6-triamine (GHPMF) at 1.9, 3.9, 7.9 and 15 µM, respectively. Also, high-pressure liquid chromatography (HPLC) analysis was run to determine the remanence of either drug in flare, and Oregon R(R)-flare flies emerged from treated larvae. S-1QN2-1 showed genotoxicity only in the ST cross, increasing the small, large and total spot frequencies at all concentrations and twin spots only at 1.9 µM; D-1 and GHPM showed significant increments of large spots only at 15 µM in the ST cross; GHPMF was not genotoxic at any concentration or either cross. In the mwh clones accumulated distribution frequencies analysis, associated with disrupted cell division, S-1QN2-1 caused alterations in the ST cross at all concentrations but only at 15 µM in the HB cross; D-1 caused alterations at 3.9, 7.9 and 15 µM in the ST cross and at 1.9 and 15 µM in the HB cross; GHPM caused alterations at 7.9 and 15 µM in the ST cross and also at 1.9, 3.9 and 7.9 µM in the HB cross; GHPMF caused those alterations at all concentrations in the ST cross and at 1.9, 3.9 and 7.9 µM in the HB cross. The HPLC results indicated no traces of either agent in the flare and Oregon R(R)-flare flies. We conclude that S-1QN2-1 is clearly genotoxic, D-1 and GHPM have an unclear genotoxicity and GHPMF was not genotoxic; all quinazoline derivatives disrupted cell division. GHPMF is a good candidate to be tested in other genotoxicity and cytotoxic bioassays. The differences in the genotoxic activity of these trypanocidal agents are correlated with differences in their chemical structure.
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