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Готові списки джерел за темами / B]thiazole

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Добірка наукової літератури з теми "B]thiazole"

Автор: Grafiati

Опубліковано: 1 липня 2022

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Статті в журналах з теми "B]thiazole"

1

Mohareb, Rafat M., Amira E. M. Abdallah, and Ebtsam A. Ahmed. "Synthesis and cytotoxicity evaluation of thiazole derivatives obtained from 2-amino-4,5,6,7-tetrahydrobenzo[b]thiophene- 3-carbonitrile." Acta Pharmaceutica 67, no. 4 (December 20, 2017): 495–510. http://dx.doi.org/10.1515/acph-2017-0040.

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Abstract Reactivity of 2-amino-4,5,6,7-tetrahydrobenzo[b]thiophene-3- carbonitrile towards thioglycolic acid resulted in thiazole derivative 1. The latter reacted with different chemical reagents to give thiazole, pyrano[2,3-d]thiazole and thiazolo[ 4,5-d]thiazole derivatives. Cytotoxicity effects of the newly synthesized products against six cancer cell lines, namely, human gastric cancer (NUGC), human colon cancer (DLD- 1), human liver cancer (HA22T and HEPG-2), human breast cancer (MCF) and nasopharyngeal carcinoma (HONE-1) as well as against a normal fibroblast cell (WI-38) were evaluated. The study showed that the 4,5,6,7 tetrahydrobenzo[ b] thiophene derivatives 6a, 7, 8a,b, 9b and 10b,c w ere t he most active compounds. Their potencies were attributed to the presence of the electron withdrawing groups.

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2

Andreani, Aldo, Mirella Rambaldi, and Alessandra Locatelli. "Herbicidal activity of 5-haloimidazo[2,1-b]thiazoles." Collection of Czechoslovak Chemical Communications 56, no. 11 (1991): 2430–35. http://dx.doi.org/10.1135/cccc19912430.

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3

Molina, Pedro, Antonio Arques, Maria de los Desamparados Velasco, and Jos� Manuel Villalgordo. "Fused Thiazoles from 3-Amino-thiazoline-2-thiones: Synthesis of Pyrazolo[5,1-b]thiazole and Thiazolo[2,3-b]-1,3,4-thiadiazine Derivatives." HETEROCYCLES 26, no. 5 (1987): 1323. http://dx.doi.org/10.3987/r-1987-05-1323.

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4

Jaberi, Hamid Reza, and Hadi Noorizadeh. "Synthesis of Some Novel Fused Imidazo [2, 1-b] [1, 3] Thiazole and Imidazo [2, 1-b] Thiazolo [5, 4-d] Isoxazole Derivatives." E-Journal of Chemistry 9, no. 3 (2012): 1518–25. http://dx.doi.org/10.1155/2012/896454.

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In this work we describe the synthesis of some novel fused imidazo [2, 1-b] [1, 3] thiazole derivatives. The reaction of 1, 2-diaminoethane 1 with carbon disulphide in H2O/ETOH as solvent furnishes 4, 5-dihydro-1H-imidazol-2-thiol 2 under reflux condition. the reaction of 4,5-dihydro-1H-imidazol-2-thiol on treatment with ethylchloro acetate and aromatic aldehyde in presence of anhydrous sodium acetate and acetic acid as solvent to give (Z)-2-(arylidene)-5,6-dihydroimidazo [2,1-b] [1,3] thiazol-3(2H)-one 3a-j. Compounds 3a-j was condensed with hydroxylamine to give 3-(aryl)-2, 3, 6, 7-tetrahydroimidazo [2, 1-b] [1,3] thiazolo [5, 4-d] isoxazole 4a-j. The structures of the new compounds were established by elemental analyses, IR,1H NMR and13C NMR data.

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5

Lan, Zheng, and Wang. "2-(3,5-Dimethyl-1H-pyrazol-1-yl)thiazolo[4,5-b]pyridine." Molbank 2019, no. 3 (August 20, 2019): M1077. http://dx.doi.org/10.3390/m1077.

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The compound 2-(3,5-dimethyl-1H-pyrazol-1-yl)thiazolo[4,5-b]pyridine (1) was synthesized with a yield of 71% by the reaction of 1-(thiazolo[4,5-b]pyridine-2-yl)hydrazine and acetylacetone. The structure was characterized by a single-crystal X-ray structure determination as well as 1H and 13C{1H} NMR spectroscopy. X-ray crystallography on 1 confirms the molecule consists of a pyridine–thiazole moiety and the pyrazole ring, and all non-hydrogen atoms are planar.

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6

Özbey, Süheyla, and Asiye Meriç. "3,4-Di-p-tolyl-6,7-dihydroimidazo[2,1-b][1,3]thiazole." Acta Crystallographica Section E Structure Reports Online 62, no. 7 (June 14, 2006): o2717—o2719. http://dx.doi.org/10.1107/s160053680602099x.

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The title compound, C19H18N2S, is a member of a new series of 2,3-dihydroimidazo[2,1-b][1,3]thiazoles and was obtained from 4,5-di-p-tolyl-1,3-dihydroimidazole-2-thione and 1-bromo-2-chloroethane. The thiazole ring adopts an envelope conformation; the plane through N, S and two C atoms makes a dihedral angle of 2.35 (3)° with the fused imidazole ring. The tolyl groups are essentially planar.

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7

El-Hagrassey, Eman A., Ehab Abdel-Latif, and Gamal M. Abdel-Fattah. "Synthesis and efficiency of new pyridine, chromene and thiazole containing compounds as antimicrobial and antioxidant agents." Bulletin of the Chemical Society of Ethiopia 36, no. 1 (March 28, 2022): 137–48. http://dx.doi.org/10.4314/bcse.v36i1.12.

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ABSTRACT. The versatile scaffold, N'-(2-cyanoacetyl)-2-hydroxybenzohydrazide (3) was utilized in the production of new pyridine, chromene and thiazole derivatives as antimicrobial and antioxidant agents. The synthetic strategy involves the treatment of precursor 3 with various arylidene-malononitrile and 3-aryl-2-cyanoacrylate compounds to furnish substituted pyridines 5 and 7. The interaction of 3 with salicylaldehyde and/or phenyl isothiocyanate followed by cyclization with chloroacetone produced the corresponding 2-imino-2H-chromene-3-carbohydrazide and (thiazol-2-ylidene-acetyl)-salicylic acid hydrazide compounds 8 and 9, respectively. The structural features of the synthesized compounds were confirmed by using spectroscopic methods such as (IR, 1H NMR, 13C NMR and MS). The new pyridine, chromene and thiazole products showed potent antioxidants and antimicrobial activities. The thiazole derivative 9 exhibited the highest anti-bacterial and antifungal activities against S. aureus (75.0%) and B. subtilis (73.9%) and C. albicans (66.6%). The combination between salicylic acid hydrazide and thiazole moieties in the hybrid 9 indicated the best antioxidant activity (87.9%). KEY WORDS: Salicylic hydrazide, Arylidene-malononitrile, Pyridine, Thiazole, Antioxidant Bull. Chem. Soc. Ethiop. 2022, 36(1), 137-148. DOI: https://dx.doi.org/10.4314/bcse.v36i1.12

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8

Shaik, Siddiq P., Telukutta S. Reddy, Satish Sunkari, Ayinampudi V. S. Rao, Korrapati S. Babu, Suresh K. Bhargava, and Ahmed Kamal. "Synthesis of Benzo[d]imidazo[2,1-b]thiazole-Propenone Conjugates as Cytotoxic and Apoptotic Inducing Agents." Anti-Cancer Agents in Medicinal Chemistry 19, no. 3 (June 25, 2019): 347–55. http://dx.doi.org/10.2174/1871520619666181127112621.

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Background: Cancer can be considered as a disease in which normal cells start behaving badly, multiplying uncontrollably, ignoring signals to stop and accumulating to form a mass that is generally termed as a tumor. Apoptosis or programmed cell death is a physiological process that enables organisms to control their cell numbers in many developmental and physiological settings and to eliminate unwanted cells and it plays essential role in chemotherapy-induced tumor-cell killing. The correct balance between apoptosis and inhibition of apoptosis is important in animal development as well as in tissue homeostasis. The aim of this paper is to introduce the readers about the design strategy and synthesis of effective cytotoxic and apoptotic inducing agents based on benzo[d]imidazo[2,1-b]thiazole scaffold. Methods: Benzo[d]imidazo[2,1-b]thiazole-propenone conjugates were synthesized by the condensation of 7- methoxy-2-(aryl)benzo[d]imidazo[2,1-b]thiazol-3-yl)prop-2-yn-1-ones with aryl/hetero aryl amines in ethanol at room temperature. These in turn were obtained from 7-methoxy-2-(aryl)benzo[d]imidazo[2,1-b]thiazole-3- carbaldehydes on treatment with ethynylmagnesium bromide followed by oxidation. Results: 3-Arylaminopropenone linked 2-arylbenzo[d]imidazo[2,1-b]thiazole conjugates prepared in this investigation exhibited significant cytotoxic activity and arrested HeLa cancer cells in G1 phase. The treatment of the conjugate led to 40% of loss of mitochondrial membrane potential (DΨm) in HeLa cells and 4 fold increase in the levels of reactive oxygen species (ROS). In addition, it induces apoptosis in HeLa cells, this was examined by the wound healing assay, Actin filaments and Hoechst staining assay. Conclusion: The encouraging biological profile exhibited by these 3-arylaminopropenone 2-aryl linked benzo[d]imidazo[2,1-b]thiazole conjugates demonstrate that they have the potential to be developed as a lead by further structural modifications to obtain potential chemotherapeutic agents that are likely to target the HeLa cancer cells.

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9

Lei, Jiaying, Xinliang Fu, Yulin Huang, and Xiaofang Li. "Synthesis of spiro[benzo[4,5]imidazo[2,1-b][1,3]thiazole-2,3-thiolane]s via sulfa-Michael/aldol cascade reactions." Journal of Chemical Research 43, no. 1-2 (January 2019): 63–66. http://dx.doi.org/10.1177/1747519819831898.

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The sulfa-Michael/aldol cascade reaction of ( Z)-2-arylmethylidene-benzo[4,5]imidazo[2,1- b]thiazol-3(2H)-ones and 1,4-dithiane-2,5-diol afforded novel 2-aryl-4-hydroxy-spiro[benzo[4,5]imidazo[2,1- b][1,3]thiazole-2,3-thiolan]-3-ones in moderate yields. The structures of all the products were characterized thoroughly by nuclear magnetic resonance, infrared and high-resolution mass spectrometry together with X-ray crystallographic analysis.

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10

Gobala Krishnan P, Gnanaprakash K, and Chandrasekhar KB. "Design, synthesis, characterization and antitubercular activity of some nov-el 2, 4-disubstituted thiazole derivatives." International Journal of Research in Pharmaceutical Sciences 10, no. 2 (April 23, 2019): 1504–9. http://dx.doi.org/10.26452/ijrps.v10i2.729.

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Literature reviews reveal that thiazole and pyrazine carboxamide derivatives exhibit anticonvulsant, antimicrobial, anticancer and anti-tubercular activities due to the presence of –S-C=N- and-CO–NH- moiety. A series of thiazolyl pyrazine carboxamide derivatives (5a-j) were synthesized by condensation reaction between 2-amino, 4-substituted phenyl 2-amino thiazole and pyrazine 2-carboxylic acid. These synthesized thiazole derivatives (5a-j) were evaluated for their inhibitory activity against Mycobacterium tuberculosis (Mtb), H37Rv using microplate Alamar Blue assay (MABA). The compound, 5c and 5h showed high anti-mycobacterial activity with MIC value of 6.25 µg/ml, and the compound 5g also exhibited anti-mycobacterial activity with MIC value of 12.50 µg/ml. Molecular docking studies of these synthesized molecules with b-Ketoacyl-ACP Synthase (KasA) protein of Mycobacterium tuberculosis (Mtb) have been carried out to understand the mechanism of anti-mycobacterial action.

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Більше джерел

Дисертації з теми "B]thiazole"

1

Ollivierre, H. M. "The synthesis and chemistry of 1,2,3-triazolo(5,1-b)thiazole." Thesis, Keele University, 1990. http://ethos.bl.uk/OrderDetails.do?uin=uk.bl.ethos.293924.

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2

Boukraa, Sadok. "Préparation, réactivité et étude des propriétés fongistatiques et immunostimulantes d'amino-2 thiazoles et d'imidazo-(2,1-B) thiazoles." Besançon, 1987. http://www.theses.fr/1987BESA2030.

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Le travail se divise en deux grandes parties : la premiere concerne la preparation d'aryl-6 imidazo(2,1-b) thiazoles substitues en 3 par des chaines de type acetate d'ethyle, aroylmethyle. (beta -hydroxy beta -aryl)ethyle te arylethyle. Pour ce faire, il a ete necessaire de preparer les amino-2 thiazoles corespondants substitues par ces memes chaines en 4 afin de las opposer a des acetophenones omega -bromees. L'influence des substituants presents est discutee en vue d'aprehender l'evolution des reactions. La seconde partie concerne des essais en tant que fongistatiques et/ou immunostimulants des composes preparees. Il ressort que les aminothiazoles sont plus interessants que les imidazothiazoles auusi bien sur l'inhibition de croissance de mycelium (epidermophyton) ou de germination des spores (candida, aspergillus) que sur la stimulation du lymphocyte t humain

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3

Le, Meur Mikaël. "Identification de nouveaux inhibiteurs de l’agrégation de la protéine Tau." Thesis, Orléans, 2014. http://www.theses.fr/2014ORLE2046.

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Parmi la vingtaine de pathologies neurodégénératives recensées à ce jour, il a été retrouvé des caractéristiques communes telles que des lésions neuronales. Dans le cas de la Maladie d’Alzheimer, une dégénérescence neurofibrillaire a notamment été mise en évidence, ce qui se traduit par l’agrégation de protéines Tau anormalement modifiées. Bien que les mécanismes moléculaires impliqués demeurent encore mal compris, nous nous sommes intéressés, au cours de cette thèse, à la synthèse puis à l’évaluation biologique de nouveaux inhibiteurs de l’agrégation de la protéine TAU impliquée dans la Maladie d’Alzheimer. Les deux premières parties de ce travail sont basées sur la conception de dérivés imidazo[2,1-b]thiazoliques, sur lesquels sont greffés un ou plusieurs groupements (hétéro)aryles. La troisième partie est, quant à elle, consacrée à la formation d’entités thiazolo[3,2-b]triazoliques di- ou trisubstituées. Le choix de ces bicycles fusionnés à cinq chainons [5,5] découle de leurs propriétés biologiques dans des domaines très variés. L’obtention de ces composés a notamment été l’occasion de mettre en oeuvre de nouvelles méthodologies de synthèses. Ainsi, sur le motif imidazo[2,1-b]thiazolique, ont été développées des réactions de couplages de Suzuki-Miyaura, des réactions multicomposants, ainsi qu’une séquence réactionnelle de condensation d’électrophiles. Sur le bicycle thiazolo[3,2-b]triazole, un travail de CH activation a également été mise au point. Une collection de deux cents moléculesoriginales a ainsi pu être constituée, et plus de la moitié des nouveaux produits ont été évalués in vitro. Unetechnique de fluorescence permettant de déterminer l’inhibition de l’agrégation des protéines TAU a été miseau point, utilisant notamment la protéine K18 comme modèle tronqué de protéine TAU
TAU pathology is a brain lesion common to more than twenty neurodegeneratives diseases. It consists of the abnormal aggregation of the microtubule-associated protein TAU into neurofibrillary tangles. While mechanisms underlying TAU aggregation are not fully understood yet, we have been investigated the synthesis and the biological evaluations of novel class of TAU aggregation inhibitors involved in Alzheimer’s disease. The first two parts of this work reports the synthesis of various imidazo[2,1-b]thiazoles molecules, on which are substituted (het)aryles groups. The third and last part is devoted to the formation of some di-/trisubstituted novel N-fused ring system such as thiazolo[3,2-b]triazoles. In order to provide a functional diversity and generate a therapeutic effect, the peaks C-2, C-3, C-5 and C-6 were functionalized on the imidazo[2,1-b]thiazole ring. It was also the opportunity to develop news synthetic methodologies such as a new Suzuki-Miyaura reaction, a multicomponent reaction, and an electrophilic condensation. On the thiazolotriazole core, an effective procedure of CH activation was performed. More than two hundred original molecules were synthesized, and more than half were evaluated in vitro. A fluorescence technique allowed us to determine the inhibition of TAU aggregation, using the particular K18 protein as a truncated model of normal TAU protein

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4

MADADI, MESSAOUD NACER. "Recherche en pharmacochimie heterocyclique antiparasitaire : pharmacomodulation de derives thiopheniques et reactions de transfert monoelectronique en serie imadazo (1,2-a) pyridine et en serie imadazo (2,1-b) thiazole." Aix-Marseille 2, 1991. http://www.theses.fr/1991AIX22956.

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5

Juspin, Thierry. "Synthèse et fonctionnalisation d'hétérocycles d'intérêt biologique par méthologie TDAE." Thesis, Aix-Marseille 2, 2010. http://www.theses.fr/2010AIX22950/document.

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Ce travail est consacré à la synthèse et à la fonctionnalisation d’hétérocycles d’intérêt biologique par méthodologie TDAE. Dans une première partie, nous avons développé la réactivité initiée par le TDAE de nouveaux électrophiles en série nitrobenzylique. L’emploi des aldéhydes-a,ß-éthyléniques et des aldéhydes hétérocycliques nous a permis d’identifier le type d’addition nucléophile de l’anion du chlorure de p-nitrobenzyle (classique ou Michael). La réaction sur une double liaison carbone-azote est possible grâce à l’emploi des iminiums quaternaires. Nous avons présenté le premier exemple de double réactivité initiée par le TDAE en faisant appel aux dialdéhydes aromatiques. Une méthodologie courte et originale nous a permis de synthétiser des quinoléines en deux étapes par association de la stratégie TDAE (avec les dicétones comme électrophiles) et de la réaction de réduction-cyclisation. Dans une deuxième partie, nous avons appliqué la méthodologie TDAE pour la découverte de composés d’intérêt pharmacologique. Après avoir synthétisé le 6-chlorométhyl-5-nitroimidazo[2,1-b]thiazole, nous avons étudié sa réactivité initiée par le TDAE avec divers a-cétoesters. Les produits obtenus ont été testés comme antibactériens et antifongiques et ont révélé une spécificité d’action sur Candida tropicalis. Dans une troisième partie, nous avons entrepris la synthèse du 4-[4-(chlorométhyl)phényl]-1,2-diméthyl-5-nitro-1H-imidazole. La réactivité initiée par le TDAE de ce substrat avec différents électrophiles (aldéhydes, a-cétoesters, dicétones) a conduit à de nouveaux alcools potentiellement actifs comme antiparasitaires notamment sur Trichomonas vaginalis
This work is focused on the synthesis and the functionalization of potentially bioactive heterocyclic compounds by TDAE methodology. In the first part, we have developed the TDAE reaction with new electrophiles in nitrobenzylic series. By using ethylenic and heterocyclic aldehydes, we have identified the kind of nucleophilic addition (classic or Michael). The reaction on a carbon-nitrogen double bond is possible with the utilization of quaternary iminiums. We have presented the first example of double TDAE-initiated reactivity with aromatic dialdehydes. A short and original methodology allows us to synthesize quinolines in a two steps TDAE-initiated reaction (using diketones as electrophiles) and reduction-cyclization reaction. In the second part, we have applied the TDAE methodology in order to discover pharmacological compounds. After synthesizing the 6-chloromethyl-5-nitroimidazo[2,1-b]thiazole, we have studied its reactivity with different a-ketoesters. All the products were tested as antibacterial and antifungal compounds; they show a specific activity against Candida tropicalis. In the third part, we synthesized the 4-[4-(chloromethyl)phenyl]-1,2-dimethyl-5-nitro-1H-imidazole. The TDAE-initiated reactivity of this substrate with different electrophiles (aldehydes, a-ketoesters, diketones) furnish new potentially bioactive alcohols as antiparasitic agents especially against Trichomonas vaginalis

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6

Boukraa, Sadok. "Préparation, réactivité et étude des propriétés fongistatiques et immunostimulantes d'amino-2 thiazoles et d'imidazo-(2,1-b) thiazoles." Grenoble 2 : ANRT, 1987. http://catalogue.bnf.fr/ark:/12148/cb376032986.

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7

Ejjoummany, Abdelaziz. "Design et fonctionnalisation d’hétérocycles originaux de type bicycliques [5-5] et tricycliques [6-5-6] à visée thérapeutique potentielle." Thesis, Orléans, 2020. http://www.theses.fr/2020ORLE3141.

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L’accès à de nouveaux composés hétérocycliques originaux biologiquement actifs, constitue l’un des principaux objectifs de notre groupe de recherche. Dans ce contexte, les travaux de cette thèse ont pour but principal, la conception de trois nouvelles familles de composés hétérocycliques contenant un motif pyrazolique susceptibles de présenter des activités biologiques, à savoir les pyrido[1',2':1,5]pyrazolo[4,3-d]pyrimidine, les pyrrolo[3,4-c]pyrazoles et les pyrazolo[5,1-b]thiazoles. Ce manuscrit est essentiellement dédié à un travail de méthodologie décrivant les différentes voies d’accès à ces hétérocycles originaux, tricycliques et bicycliques potentiellement modulables. La réactivité de ces synthons clés est ensuite étudiée avec divers procédés de fonctionnalisation palladocatalysés (Activation au PyBrOP-(hétéro)arylation, Liebeskind-Srogl, Suzuki-Miyaura, Buchwald-Hartwig, C-H arylation, substitution nucléophile aromatique) pour élaborer d’intéressantes chimiothèques construites autour de ces structures inédites, ouvrant ainsi de nombreuses perspectives pharmacologiques
The access to new original biologically active heterocyclic compounds, is one of the main objectives of our research group. In this context, the main purpose of this thesis is the design of three new families of heterocyclic compounds containing a pyrazolic motif that may exhibit biological activities, namely pyrido[1',2': 1.5]pyrazolo[4,3-d]pyrimidine, pyrrolo[3,4-c]pyrazole and pyrazolo[5,1-b]thiazole.This manuscript is essentially dedicated to a methodology work describing the different routes of access to these originals and potentially modular tricyclic and bicyclic precursors. The reactivity of these key synthons is then studied towards aromatic nucleophilic substitutions reactions and various pallado-catalyzed methods of functionalization (Activation with PyBrOP- (hetero) arylation, Liebeskind-Srogl, Suzuki-Miyaura, Buchwald-Hartwig, C-H arylation, aromatic nucleophilic substitution) to develop interesting libraries built around these unusual structures, thus opening numerous pharmacological perspectives

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8

Chew, Angela Christine. "The anti-proliferative effects of thiazolidinediones and non-steriodal anti-inflammatory drugs on androgen-independent prostate cancer." University of Western Australia. School of Medicine and Pharmacology, 2009. http://theses.library.uwa.edu.au/adt-WU2009.0200.

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[Truncated abstract] In recent years a better understanding of the biology of PPAR , a nuclear transcription factor, has emerged, leading to a resurgence in targeting PPAR for chemotherapy. The family of synthetic PPAR agonists, the thiazolidinediones (TZDs), and non-steroidal anti-inflammatory drugs (NSAIDs) have been implicated in the inhibition of cell proliferation, apoptosis and cell cycle arrest of androgen-sensitive (LNCaP) and androgen-independent (PC-3 and DU145) prostate cancer cells generating much interest in their use for potential curative cancer therapies. In light of the potential use of TZDs and NSAIDs in prostate cancer prevention and their ability to induce inhibitory effects in vitro and in vivo, the first aim of this project was to undertake a comprehensive study of the effects of ciglitazone (TZD) and indomethacin (NSAID) on the androgen-independent prostate cancer cell line DU145, using standardised concentrations and time-points to compare the effects of TZDs and NSAIDs on cell proliferation, cell cycle and apoptosis. Treating the cells with either 10 µM ciglitazone or 10 µM indomethacin resulted in a time-dependent decrease in DU145 cell proliferation. The anti-proliferative effects were found to be in-part attributed to the slowing of cell progression through the G1/S-phase checkpoint of the cell cycle, and in the case of ciglitazone, apoptosis also played a role in its anti-proliferative effects in this cell line. Interestingly, although indomethacin failed to induce apoptosis, its antiproliferative effects were more potent than ciglitazone. The second aim of this project was to further investigate the underlying mechanisms responsible for the anti-proliferative effects of ciglitazone and indomethacin by evaluating their ability to modulate PPAR mRNA and protein expression, and to induce PPAR transcriptional activity. ... In addition, ligandinduced regulation of secreted frizzled related protein 4 (sFRP4) expression, a Wnt/ - catenin antagonists, was investigated. It was demonstrated that both ciglitazone and indomethacin attenuated Wnt/ -catenin signalling via the down-regulation of total - catenin levels within the cells, inhibition or slowing of the translocation of cytoplasmic -catenin into the nucleus and inhibition of cyclinD1 expression An inverse relationship between PPAR and -catenin protein levels was also detected, suggesting that PPAR may directly bind to -catenin itself. sFRP4 expression was transiently upregulated by ciglitazone and indomethacin-treatment, suggesting that the antiproliferative effects of the ligands may be mediated in part through regulation of sFRP4 mRNA and protein levels. In summary, the anti-proliferative effects of ciglitazone and indomethacin on the androgen-independent prostate cancer cell line, DU145, described in this thesis are progressive steps in characterising the role of PPAR in prostate cancer cell proliferation. The identification of indomethacin as a more potent PPAR agonist than ciglitazone represents a novel target for the development of preventative strategies for advanced disease, and the relationship between PPAR and the Wnt/ -catenin signalling pathway provide an insight into the mechanisms involved in the anti-proliferative effects of ciglitazone and indomethacin. Further studies into this relationship would advance help identify novel preventative and curative therapeutic strategies for advanced prostate cancer.

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Kalyon, Bahar [Verfasser], Roderich [Akademischer Betreuer] SüßMuth, and Hans-Peter [Akademischer Betreuer] Fiedler. "Fermentation, Isolierung und Strukturaufklärung der ribosomal synthetisierten Thiazol/Oxazol-Peptide Plantazolicin A und B aus Bacillus amyloliquefaciens FZB42 und Strukturaufklärung der Langkocycline aus Streptomyces sp. Acta 3034 / Bahar Kalyon. Gutachter: Roderich Süßmuth ; Hans-Peter Fiedler." Berlin : Technische Universität Berlin, 2014. http://d-nb.info/1067384782/34.

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10

Almeida, Mário Rui Dias. "Synthesis of 5-aryl-imidazo [2,1-b] thiazole compounds possibly RAF kinase inhibitors." Master's thesis, 2014. http://hdl.handle.net/10451/38753.

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Trabalho Final de Mestrado Integrado, Ciências Farmacêuticas, Universidade de Lisboa, Faculdade de Farmácia, 2014
Malignant melanoma is the most aggressive type of skin cancer because of its high tendency to metastasize. In fact, the mortality rate from malignant melanoma has risen about 2% annually since 1960. Malignant melanoma occupies the 19th place as the most common cancer worldwide. In Portugal, according to the Portuguese League Against Cancer are nearly 700 new cases of melanoma annually and the incidence rate reaches 6-8 cases per 100000 individuals. These data are similar to South European countries, namely, Spain and Italy. There are several options of treatments for malignant melanoma and the right choice depends of several aspects, being the most important one, the actual stage of the cancer. The understanding of carcinogenesis’ mechanisms at the molecular level has led to the opportunity of development new therapeutic approaches. Recently, some pyrimidinyl substituted imidazo[2,1-b]thiazole derivatives were reported as RAF kinases inhibitors. Therefore, these compounds provide a broad and novel opportunity to treat melanoma, which should be further investigated. The obtained compounds, showing promising proprieties, will be further investigated to evaluate its pharmacokinetic and toxicokinetic proprieties in biological assays performed in several melanoma cultured cells.
O melanoma maligno é o tipo de cancro de pele mais grave devido à sua alta tendência para metastizar. Desde 1960, a sua taxa de mortalidade tem aumentado cerca de 2% anualmente. O melanoma maligno ocupa o 19º lugar entre os cancros mais comuns a nível mundial. Em Portugal, de acordo com a Liga Portuguesa Contra o Cancro existem cerca de 700 novos casos de melanoma por ano e a taxa de incidência de melanoma é de 6-8 casos por 100000 pessoas, bastante similar aos países do Sul da Europa, nomeadamente Espanha e Itália. Existem várias opções terapêuticas para o melanoma maligno, no entanto, a escolha mais adequada depende de vários fatores, sendo o mais importante, o estadio do cancro. A compreensão dos mecanismos de carcinogénese, numa perspetiva molecular, permitiu o desenvolvimento de novas opções terapêuticas. Recentemente, alguns derivados imidazo[2,1-b]tiazólicos com grupos pirimidínicos substituídos foram descritos como inibidores das quinases RAF. Consequentemente, estes compostos permitem uma inovadora modalidade de tratamento do melanoma que deve ser explorada. Os compostos sintetizados neste trabalho, caso sejam realmente promissores, serão investigados mais aprofundadamente, para avaliar as suas propriedades farmacocinéticas e toxicodinâmicas em ensaios biológicos realizados em diversas linhas celulares de melanoma.

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Частини книг з теми "B]thiazole"

1

Forti, G. Cantelli, P. Hrelia, M. C. Guerra, M. Paolini, A. M. Barbaro, and G. L. Biagi. "Genotoxic Activity of Nitroimidazo(2,1-b)Thiazole Derivatives in Salmonella Typhimurium and Saccharomyces Cerevisiae Assays." In Archives of Toxicology, 408. Berlin, Heidelberg: Springer Berlin Heidelberg, 1985. http://dx.doi.org/10.1007/978-3-642-69928-3_89.

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2

Hegde, Shridhar G., Martin D. Mahoney, and Claude R. Jones. "Thiazolo[4,5-b]pyridine-3(2H)-acetic Acid Derivatives." In ACS Symposium Series, 70–77. Washington, DC: American Chemical Society, 1995. http://dx.doi.org/10.1021/bk-1995-0584.ch007.

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3

Biagi, G. L., P. Hrelia, M. C. Guerra, M. Paolini, A. M. Barbaro, and G. Cantelli-Forti. "Structure-Activity Relationshipof Nitroimidazo (2,1-b) Thiazoles in the Salmonella Mutagenicity Assay." In Archives of Toxicology, 425–29. Berlin, Heidelberg: Springer Berlin Heidelberg, 1986. http://dx.doi.org/10.1007/978-3-642-71248-7_86.

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4

"2,3-Dihydro-7H-pyrido[2,1-b]-1,3-thiazole." In Substance Index, edited by Backes, Fröhlich, and Padeken. Stuttgart: Georg Thieme Verlag, 2000. http://dx.doi.org/10.1055/b-0035-114034.

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5

"1,3-Thiazole(I)." In Substance Index, edited by Backes, Fröhlich, and Pedeken. Stuttgart: Georg Thieme Verlag, 1999. http://dx.doi.org/10.1055/b-0035-114060.

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"1,3-Thiazole(II)." In Substance Index, edited by Backes, Fröhlich, and Pedeken. Stuttgart: Georg Thieme Verlag, 1999. http://dx.doi.org/10.1055/b-0035-114061.

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7

"Tetrahydro-1,3-thiazole, 1,3-Thiazolidine to 4,5-Dihydro-1,3-thiazolium." In Substance Index, edited by Backes, Fröhlich, and Pedeken. Stuttgart: Georg Thieme Verlag, 1999. http://dx.doi.org/10.1055/b-0035-114059.

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8

Sammakia, Tarek, Eric L. Stangeland, and Mark C. Whitcomb. "Chapter 13 Functionalization of pyridines and thiazoles via the halogen-dance reaction, application to the total synthesis of caerulomycin c and WS75624 B." In Strategies and Tactics in Organic Synthesis, 415–36. Elsevier, 2005. http://dx.doi.org/10.1016/s1874-6004(05)80036-x.

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Тези доповідей конференцій з теми "B]thiazole"

1

Nikhila, G. R., S. R. Batakurki, and B. C. Yallur. "Synthesis, characterization and antioxidant studies of benzo[4, 5]imidazo[2, 1-b]thiazole derivatives." In PROCEEDINGS OF INTERNATIONAL CONFERENCE ON ADVANCES IN MATERIALS RESEARCH (ICAMR - 2019). AIP Publishing, 2020. http://dx.doi.org/10.1063/5.0023101.

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2

Al-Jamal, Mazin H., Naeemah Al-Lami, and Ruqia M. Al-Azy. "Synthesis of new S, N, O-alkylated benzo [d] imidazo [2,1-b]thiazole and the study of their biological applications." In 2ND INTERNATIONAL CONFERENCE ON MATERIALS ENGINEERING & SCIENCE (IConMEAS 2019). AIP Publishing, 2020. http://dx.doi.org/10.1063/5.0000174.

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3

Fidanze, Steve D., Scott A. Erickson, Robert D. Hubbard, Gary T. Wang, Robert A. Mantei, Nwe Y. BaMaung, Richard F. Clark, et al. "Abstract A245: Imidazo[2,1‐b]thiazole and imidazo[1,2‐a]pyridine amides as novel inhibitors of the insulin‐like growth factor (IGF1R) and members of the epidermal growth factor family of tyrosine kinases." In Abstracts: AACR-NCI-EORTC International Conference: Molecular Targets and Cancer Therapeutics--Nov 15-19, 2009; Boston, MA. American Association for Cancer Research, 2009. http://dx.doi.org/10.1158/1535-7163.targ-09-a245.

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