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Journal articles on the topic 'Antiproliferative properties'

Author: Grafiati

Published: 18 May 2024

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1

Yoshizawa, Yuko, Kenji Sakurai, Satoru Kawaii, Masayoshi Asari, Junichi Soejima, and Noboru Murofushi. "Comparison of Antiproliferative and Antioxidant Properties among Nineteen Apple Cultivars." HortScience 40, no. 5 (August 2005): 1204–7. http://dx.doi.org/10.21273/hortsci.40.5.1204.

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Aqueous ethanol extracts prepared from 19 apple (Malus ×domestica Borkh.) cultivars were studied to explore their antiproliferative activity. Half of them showed strong inhibition on proliferation of human leukemic HL-60 cells, while the others were weak. Total polyphenols, 1, 1-diphenyl-2-picrylhydrazyl (DPPH) radical scavenging activity, and total anthocyanins were measured and the results indicated that the antiproliferative activity was more strongly correlated to the polyphenols and radical scavenging activity than to the anthocyanin content. Several polyphenols in `Jonathan' were identified and quantified by high-performance liquid chromatography (HPLC) analysis. Among those compounds found during HPLC, catechin and epicatechin seemed partially responsible for HL-60 antiproliferation. A careful examination on parentage of the apple cultivars tested revealed that `Jonathan' and its progeny showed high antiproliferation toward HL-60. This is the first observation about the relationship between antiproliferative activity and parentage of apples, and the information would be useful to create new apple cultivars that posses more anticancer potential.

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2

Liu, Xiaoling, and Mei-Lin Go. "Antiproliferative properties of piperidinylchalcones." Bioorganic & Medicinal Chemistry 14, no. 1 (January 2006): 153–63. http://dx.doi.org/10.1016/j.bmc.2005.08.006.

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3

Kessler, Romain, Serge Dumont, Emmanuel Weitzenblum, and Philippe Poindron. "Antiproliferative Properties of Human Alveolar Macrophages." Respiration 65, no. 5 (1998): 363–68. http://dx.doi.org/10.1159/000029296.

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4

Çankaya, Nevin. "Synthesis of Hydrogels Containing Halloysite and Investigation of Antiproliferative Activity." Advances in Clinical Toxicology 8, no. 3 (2023): 1–10. http://dx.doi.org/10.23880/act-16000274.

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In this study, superabsorbent hydrogels containing halloysite clay, biopolymer (CMC, carboxymethyl cellulose), acrylamide (AM) and 2-acrylamido-2-methyl-1-propanesulfonic acid (AMPS) were synthesized and characterized by free radical polymerization method. Then, the cytotoxic effect of hydrogels on MDA-MB-231 breast cancer cells was evaluated. According to the findings, hydrogels were successfully synthesized and their cytotoxic properties were supported by in vitro studies. In order for these hydrogels to be used as a drug delivery system, their potential properties need to be supported by further research such as in vivo.

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YOSHIZAWA, Yuko, Kenji SAKURAI, Satoru KAWAII, Junichi SOEJIMA, and Noboru MUROFUSHI. "Antiproliferative and Antioxidant Properties of Crabapple Juices." Food Science and Technology Research 10, no. 3 (2004): 278–81. http://dx.doi.org/10.3136/fstr.10.278.

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6

Recio, Mari-Carmen, Rosa-María Giner, and Salvador Máñez. "Immunmodulatory and Antiproliferative Properties of Rhodiola Species." Planta Medica 82, no. 11/12 (May 25, 2016): 952–60. http://dx.doi.org/10.1055/s-0042-107254.

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7

Gescher, Andreas. "Antiproliferative properties of phorbol ester tumour promoters." Biochemical Pharmacology 34, no. 15 (August 1985): 2587–92. http://dx.doi.org/10.1016/0006-2952(85)90552-0.

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8

Trindade, Cristiano, André Luiz Mendes Juchem, Temenouga N. Guecheva, Iuri M. de Oliveira, Priscila dos Santos Silveira, José Eduardo Vargas, Renato Puga, Claudia Ó. Pessoa, and João A. P. Henriques. "Diphenyl Ditelluride: Redox-Modulating and Antiproliferative Properties." Oxidative Medicine and Cellular Longevity 2019 (October 24, 2019): 1–14. http://dx.doi.org/10.1155/2019/2510936.

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Tellurium is a rare element that has been regarded as a toxic, nonessential element, and its biological role is not clearly established. In addition, the biological effects of elemental tellurium and some of its organic and inorganic derivatives have been studied, leading to a set of interesting and promising applications. Diphenyl ditelluride (DPDT), an organic tellurium derivate, showed antioxidant, antigenotoxic, antimutagenic, and anticancer properties. The antioxidant and prooxidant properties of DPDT are complex and depend on experimental conditions, which may explain the contradictory reports of these properties. In addition, DPDT may exert its effects through different pathways, including distinct ones to those responsible for chemotherapy resistance phenotypes: transcription factors, membrane receptors, adhesion, structural molecules, cell cycle regulatory components, and apoptosis pathways. This review aims to present recent advances in our understanding of the biological effects, therapeutic potential, and safety of DPDT treatment. Moreover, original results demonstrating the cytotoxic effects of DPDT in different mammalian cell lines and systems biology analysis are included, and emerging approaches for possible future applications are inferred.

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9

Sousa, André, Paula Araújo, Joana Azevedo, Luís Cruz, Iva Fernandes, Nuno Mateus, and Victor de Freitas. "Antioxidant and antiproliferative properties of 3-deoxyanthocyanidins." Food Chemistry 192 (February 2016): 142–48. http://dx.doi.org/10.1016/j.foodchem.2015.06.108.

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10

Boratyński, Przemysław J., Joanna Gałęzowska, Kamil Turkowiak, Artur Anisiewicz, Rafał Kowalczyk, and Joanna Wietrzyk. "Triazole Biheterocycles fromCinchonaAlkaloids: Coordination and Antiproliferative Properties." ChemistrySelect 3, no. 32 (August 29, 2018): 9368–73. http://dx.doi.org/10.1002/slct.201801810.

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11

Kin, Min, and Ji Kim. "Phytochemicals, Antioxidant and Anticancer Properties of Camellia japonica L. Mistletoe Extracts." Journal of Tropical Life Science 12, no. 2 (May 17, 2022): 269–74. http://dx.doi.org/10.11594/jtls.12.02.13.

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The present study aims to investigate the phytochemical profiles, in vitro antioxidant and antiproliferative properties of methanol and 70% ethanol extracts of Camellia mistletoe. Both extracts were analyzed for contents of total flavonoid, total carotenoid and L-ascorbic acid, and antioxidant properties such as scavenging capacities (1,1-diphenyl-2-picrylhydrazyl, O2- and NO), ferrous ion chelating and reducing power. MTT assay was used to assess the antiproliferative properties against human cancer cell lines. The results showed that the methanol extracts of Camellia mistletoe contained higher total flavonoids (16237 mg rutin equivalents/100 g) and carotenoids (49175 mg/100g) with higher DPPH (IC50 = 0.6 mg/mL), superoxide (IC50 = 0.6 mg/mL), nitric oxide (IC50 = 0.5 mg/mL) radical scavenging and reducing power (IC50 = 1.1 mg/mL) activities than those of ethanol extracts (p < 0.05). In addition, methanol extracts showed much higher antiproliferative activity against A375 (IC50 = 118.1 μg/mL) and HCT116 (IC50 = 148.4 μg/mL) cells than ethanol extracts whereas higher inhibitory effects of MCF7 (IC50 = 139.9 μg/mL), Hela (IC50 = 127.1 μg/mL) and HepG2 (IC50 = 84.2 μg/mL) cell proliferation in the ethanol extracts of Camellia mistletoe. The data from this study suggest that Camellia mistletoe is a potential source of phytochemical compounds with antioxidant and antiproliferative properties.

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12

Marques, Beatriz C., Mariana B. Santos, Daiane B. Anselmo, Diego A. Monteiro, Eleni Gomes, Marilia F. C. Saiki, Paula Rahal, Pedro L. Rosalen, Janaina C. O. Sardi, and Luis O. Regasini. "Methoxychalcones: Effect of Methoxyl Group on the Antifungal, Antibacterial and Antiproliferative Activities." Medicinal Chemistry 16, no. 7 (November 6, 2020): 881–91. http://dx.doi.org/10.2174/1573406415666190724145158.

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Background: Chalcones substituted by methoxyl groups have presented a broad spectrum of bioactivities, including antifungal, antibacterial and antiproliferative effects. However, a clear and unambiguous investigation about the relevance of this substituent on the chalcone framework has not been described. Objective: The purpose of this work is to assess the antibacterial, antifungal and antiproliferative activities of the two series of seventeen synthesized regioisomeric methoxychalcones. Series I and II were constituted by chalcones substituted by methoxyl groups on rings A (5–12) and B (13–21), respectively. In addition, the library of methoxychalcones was submitted to in silico drug-likeness and pharmacokinetics properties predictions. Methods: Methoxychalcones were synthesized and their structures were confirmed by NMR spectral data analyses. Evaluations of antimicrobial activity were performed against five species of Candida, two Gram-negative and five Gram-positive species. For antiproliferative activity, methoxychalcones were evaluated against four human tumorigenic cell lines, as well as human non-tumorigenic keratinocytes. Drug-likeness and pharmacokinetics properties were predicted using Molinspiration and PreADMET toolkits. Results: In general, chalcones of series I are the most potent antifungal, antibacterial and antiproliferative agents. 3’, 4’, 5’-Trimethoxychalcone (12) demonstrated potent antifungal activity against Candida krusei (MIC = 3.9 μg/mL), eight times more potent than fluconazole (reference antifungal drug). 3’-Methoxychalcone (6) displayed anti-Pseudomonas activity (MIC = 7.8 μg/mL). 2’,5’-Dimethoxychalcone (9) displayed potent antiproliferative effect against C-33A (cervix), A-431 (skin) and MCF-7 (breast), with IC50 values ranging from 7.7 to 9.2 μM. Its potency was superior to curcumin (reference antiproliferative compound), which exhibited IC50 values ranging from 10.4 to 19.0 μM. Conclusion: Our studies corroborated the relevance of methoxychalcones as antifungal, antibacterial and antiproliferative agents. In addition, we elucidated influence of the position and number of methoxyl groups toward bioactivity. In silico predictions indicated good drug-likeness and pharmacokinetics properties to the library of methoxychalcones.

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13

Jackson, Joshua, Gerome M. Romero, Diana Hawkins, Richard G. Cornwall, and Georgi L. Lukov. "Identifying the Structural Components Responsible for the Antiproliferative Properties of Hydroxychavicol." Compounds 3, no. 4 (October 25, 2023): 552–60. http://dx.doi.org/10.3390/compounds3040039.

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Betel leaves are widely used as herbal medicine in Asia due to their antimicrobial properties. These properties have been attributed to the phenolic compound eugenol and its derivative, hydroxychavicol. Hydroxychavicol has also been shown to inhibit cancer cell proliferation. The main objective of this study was to investigate which structural components of hydroxychavicol are responsible for the antiproliferative property of this compound. Jurkat-E6 cells (JE6) were treated with increasing concentrations (5, 15, and 45 µM) of hydroxychavicol and structural variants of it for 48 h. The results of this study demonstrate that the catechol structure in hydroxychavicol is the structural component that exhibits the highest antiproliferative effect. More specifically, the data show that the six-carbon ring must be aromatic with the two hydroxyl groups attached in an ortho position. Furthermore, this study establishes that the oxygen in the hydroxyl groups has a vital role in the antiproliferative properties of catechol and hydroxychavicol.

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14

Wróbel, Tomasz M., Michał Kiełbus, Agnieszka A. Kaczor, Vladimír Kryštof, Zbigniew Karczmarzyk, Waldemar Wysocki, Andrzej Fruziński, et al. "Discovery of nitroaryl urea derivatives with antiproliferative properties." Journal of Enzyme Inhibition and Medicinal Chemistry 31, no. 4 (June 26, 2015): 608–18. http://dx.doi.org/10.3109/14756366.2015.1057716.

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15

Na, Eun, Jung Woo Lee, Stefan Winkler, and Sun Young Lim. "Antiproliferative Properties of Extracts from Stachys sieboldii MIQ." Current Bioactive Compounds 16, no. 3 (June 10, 2020): 342–47. http://dx.doi.org/10.2174/1573407214666181112111257.

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Background: The objective of this study was to investigate the antiproliferative effect of Stachys sieboldii MIQ. extracts on cancer cell lines. Methods: Dried S. sieboldii MIQ. was extracted using acetone/methylene chloride (A+M) or methanol (MeOH), and then fractionated using n-hexane, 85% aq. methanol (MeOH), butanol (BuOH) and distilled water. The cytotoxic activity of S. sieboldii MIQ. against AGS human gastric, HT-29 human colon and HT-1080 fibroblast cancer cell lines was assessed using the 3-(4,5-dimethylthiazol-2-yl)-2,5- diphenyltetrazolium bromide (MTT) assay. Results: The A+M extract showed significantly higher inhibition of cell growth in all three cell lines compared to the MeOH extract (p < 0.05). All the extracts and fractions from S. sieboldii MIQ. decreased the growth of AGS cells, and the effect was concentration-dependent. Among the different fractions, the n-Hexane and 85% aq. MeOH fractions inhibited AGS cell growth by >50% at a concentration of 0.1 mg/mL (p < 0.05). All fractions inhibited the proliferation of HT-29 cancer cell lines (p < 0.05), showing >50% inhibition at a concentration of 0.25 mg/mL. The A+M extract inhibited the growth of the HT-1080 cancer cells by 60% at a concentration of 0.25 mg/mL. The n-Hexane and 85% aq. MeOH fractions showed the highest growth inhibitory effect on the HT-1080 cancer cells (p < 0.05), similar to that observed in the AGS cancer cells. Conclusion: Thus, the n-Hexane and 85% aq. MeOH fractions from S. sieboldii MIQ. likely contain bioactive compounds such as polyphenols and flavonoids that could prevent cancer proliferation. Further research is needed to isolate these important compounds from the extracts.

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16

Tavares, L., S. Fortalezas, C. Carrilho, G. J. McDougall, D. Stewart, R. B. Ferreira, and C. N. Santos. "Antioxidant and antiproliferative properties of strawberry tree tissues." Journal of Berry Research 1, no. 1 (2010): 3–12. http://dx.doi.org/10.3233/br-2010-001.

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17

Martynov, A. V., and M. V. Smelyanskaya. "Antiproliferative Properties of Chemically Modified Recombinant IFN-α2b." Journal of Interferon & Cytokine Research 25, no. 7 (July 2005): 414–17. http://dx.doi.org/10.1089/jir.2005.25.414.

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18

Moran, Jose M., Olga Leal-Hernandez, Maria L. Canal-Macías, Raul Roncero-Martin, Rafael Guerrero-Bonmatty, Ignacio Aliaga, and Juan D. Pedrera Zamorano. "Antiproliferative Properties of Oleuropein in Human Osteosarcoma Cells." Natural Product Communications 11, no. 4 (April 2016): 1934578X1601100. http://dx.doi.org/10.1177/1934578x1601100418.

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In this study, we evaluated the antiproliferative activity on two human osteosarcoma cell lines (MG-63 and Saos2) of oleuropein, an olive oil compound traditionally found in the Mediterranean diet. Oleuropein exhibited obvious cytotoxic effects on human osteosarcoma cells in a concentration- and time-dependent manner. Statistical analysis of IC50 by the Probit regression method suggested that oleuropein had similar toxic effects on both cell lines tested (IC50 range from 247.4–475.0 μM for MG63 cells and from 798.7–359.9 μM for Saos2 cells).

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19

Fedorov, Alexey, Iuliia Gracheva, Elena Svirshchevskaya, Vladimir Faerman, and Irina Beletskaya. "Synthesis and Antiproliferative Properties of Bifunctional Allocolchicine Derivatives." Synthesis 50, no. 14 (May 28, 2018): 2753–60. http://dx.doi.org/10.1055/s-0037-1610146.

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Based on the natural antimitotic agent colchifoline as a lead structure, a series of novel bifunctional allocolchicine congeners were synthesized from commercial colchicine. The new derivatives maintain good cytotoxicity against T3M4, MiaPaCa-2, and PANC-1 cell lines. The presence of functional groups simplifies further modifications of the prepared structures and the design of novel colchicine-derived antitumor compounds with desired pharmacological properties.

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20

Dalla Via, Lisa, Jose Carlos González-Gómez, Lázaro Guillermo Pérez-Montoto, Lourdes Santana, Eugenio Uriarte, Sebastiano Marciani Magno, and Ornella Gia. "A new psoralen derivative with enlarged antiproliferative properties." Bioorganic & Medicinal Chemistry Letters 19, no. 10 (May 2009): 2874–76. http://dx.doi.org/10.1016/j.bmcl.2009.03.073.

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21

Liu, Su-You, Jiang Zeng, Kun-Jian Peng, Li-Chao Zhang, Li-Jun Liu, Zhi-Yong Luo, and Da-You Ma. "Synthesis and antiproliferative properties of novel naringenin derivatives." Medicinal Chemistry Research 26, no. 10 (July 11, 2017): 2692–98. http://dx.doi.org/10.1007/s00044-017-1966-y.

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22

Denny, Carina, Marcela Engelbrecht Zacharias, Ana Lúcia Tasca Gois Ruiz, Maria do Carmo E. do Amaral, Volker Bittrich, Luciana Konecny Kohn, Ilza Maria de Oliveira Sousa, Rodney Alexandre Ferreira Rodrigues, João Ernesto de Carvalho, and Mary Ann Foglio. "Antiproliferative properties of polyketides isolated fromVirola sebifera leaves." Phytotherapy Research 22, no. 1 (2007): 127–30. http://dx.doi.org/10.1002/ptr.2251.

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23

Mojžišová, Gabriela, Ján Mojžiš, Martina Pilátová, Lenka Varinská, Lenka Ivanová, Ladislav Strojný, and Ján Richnavský. "Antiproliferative and Antiangiogenic Properties of Horse Chestnut Extract." Phytotherapy Research 27, no. 2 (March 26, 2012): 159–65. http://dx.doi.org/10.1002/ptr.4688.

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24

Karaguni, Ioanna-Maria, Karl-Heinz Gluesenkamp, Anette Langerak, Christoph Geisen, Volker Ullrich, Guenther Winde, Tarik Moeroey, and Oliver Mueller. "ChemInform Abstract: New Indene-Derivatives with Antiproliferative Properties." ChemInform 33, no. 21 (May 21, 2010): no. http://dx.doi.org/10.1002/chin.200221075.

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25

Hu, Renqiu, Joseph Bekisz, Mark Hayes, Susette Audet, Judy Beeler, Emanuel Petricoin, and Kathryn Zoon. "Divergence of Binding, Signaling, and Biological Responses to Recombinant Human Hybrid IFN." Journal of Immunology 163, no. 2 (July 15, 1999): 854–60. http://dx.doi.org/10.4049/jimmunol.163.2.854.

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Abstract Three human IFN-α hybrids, HY-1 [IFN-α21a(1-75)/α2c(76-165)], HY-2 [IFN-α21a(1-95)/α2c(96-165)], and HY-3 [IFN-α2c(1-95)/α21a(96-166)], were constructed, cloned, and expressed. The hybrids had comparable specific antiviral activities on Madin-Darby bovine kidney (MDBK)3 cells but exhibited very different antiproliferative and binding properties on human Daudi and WISH cells and primary human lymphocytes. Our data suggest that a portion of the N-terminal region of the molecule is important for interaction with components involved in binding of IFN-α2b while the C-terminal portion of IFN is critical for antiproliferative activity. A domain affecting the antiproliferative activity was found within the C-terminal region from amino acid residues 75–166. The signal transduction properties of HY-2 and HY-3 were evaluated by EMSA and RNase protection assays. Both HY-2 and HY-3 induced activation of STAT1 and 2. However, HY-2 exhibited essentially no antiproliferative effects at concentrations that activated STAT1 and 2. Additionally, at concentrations where no antiproliferative activity was seen, HY-2 induced a variety of IFN-responsive genes to the same degree as HY-3. RNase protection assays also indicate that, at concentrations where no antiproliferative activity was seen for HY-2, this construct retained the ability to induce a variety of IFN-inducible genes. These data suggest that the antiproliferative response may not be solely directed by the activation of the STAT1 and STAT2 pathway in the cells tested.

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26

Elo, Hannu, and Paavo Lumme. "Antiproliferative Activity of Derivatives of trans-Bis(salicylaldoximato)copper(II) in vitro. Some in vivo Properties of the Parent Compound." Zeitschrift für Naturforschung C 41, no. 9-10 (October 1, 1986): 951–55. http://dx.doi.org/10.1515/znc-1986-9-1024.

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Several derivatives and analogs of the recently reported antiproliferative and antitumor agent trans-bis(salicylaldoximato) copper(II) (CuSAO2) have been prepared and tested for antiproliferative activity against L1210 leukemia cells in vitro. The salicylaldimine analog of CuSAO2 had a very strong antiproliferative activity, the 2-day IC50 value being lower than 3 μg/ml- The 2,3-dihydroxybenzaldoxime analog was equally active with CuSAO2, while the corresponding 2,5-dihydroxy derivative had a slightly lower activity. The 2,3,4-trihydroxybenzaldoxime derivative had a much lower activity than had the dihydroxybenzaldoxime derivatives. The zinc(II) analog of CuSAO2 had only a low antiproliferative activity. The ligand of CuSAO2, salicylaldoxime, resembles pyridoxal oxime, a vitamin B6 antagonist and a powerful inhibitor of pyridoxal kinase. An attempt to reduce the toxicity of CuSAO2 in vivo with pyridoxal hydrochloride led to increased toxicity.

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27

Leyva-Peralta, Mario A., Ramón E. Robles-Zepeda, Rodrigo S. Razo-Hernández, Laura P. Á. Berber, Karen O. Lara, Eduardo Ruiz-Bustos, and Juan C. Gálvez-Ruíz. "Berberine as Source of Antiproliferative Hybrid Compounds: In Vitro Antiproliferative Activity and Quantitative Structure-activity Relationship." Anti-Cancer Agents in Medicinal Chemistry 19, no. 15 (January 10, 2019): 1820–34. http://dx.doi.org/10.2174/1871520619666190503121820.

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Background: Despite advances for cancer treatment, it still remains a major worldwide public health problem. Compounds derived from natural sources are important alternatives to combat this mortal disease. Berberine is an isoquinoline alkaloid with a wide variety of pharmacological properties, including antiproliferative activity. Previously, we have found that fatty acids also show antiproliferative activity against cancer cell lines. Background: Despite advances for cancer treatment, it still remains a major worldwide public health problem. Compounds derived from natural sources are important alternatives to combat this mortal disease. Berberine is an isoquinoline alkaloid with a wide variety of pharmacological properties, including antiproliferative activity. Previously, we have found that fatty acids also show antiproliferative activity against cancer cell lines. Objective: To combine berberine and fatty acids, or carboxylic acids, in order to improve their antiproliferative properties. Objective: To combine berberine and fatty acids, or carboxylic acids, in order to improve their antiproliferative properties. Methods: We synthetized six new hybrid derivatives through a simple methylenedioxy group-cleavage method followed by the reaction with fatty acids, or carboxylic acids. The structure of the compounds was elucidated by IR, NMR and HRMS. The in vitro antiproliferative activity against four human cancer cell lines (HeLa, A-549, PC-3 and LS-180) and one normal cell line (ARPE-19), was evaluated by the MTT method. Chemical structures were drawn using SPARTAN '08 software and the conformational analysis was carried out with a molecular mechanic level of theory and the SYBIL force field. All molecular structures were subjected to geometrical optimization at the semi-empirical method PM3. Molecular descriptors were calculated using DRAGON 5.4 and SPARTAN ´08 programs. Methods: We synthetized six new hybrid derivatives through a simple methylenedioxy group-cleavage method followed by the reaction with fatty acids, or carboxylic acids. The structure of the compounds was elucidated by IR, NMR and HRMS. The in vitro antiproliferative activity against four human cancer cell lines (HeLa, A-549, PC-3 and LS-180) and one normal cell line (ARPE-19), was evaluated by the MTT method. Chemical structures were drawn using SPARTAN '08 software and the conformational analysis was carried out with a molecular mechanic level of theory and the SYBIL force field. All molecular structures were subjected to geometrical optimization at the semi-empirical method PM3. Molecular descriptors were calculated using DRAGON 5.4 and SPARTAN ´08 programs. Results: The geranic acid and berberine hybrid compound (6) improved the antiproliferative activity shown by natural berberine, even more than the 16- to 18-carbon atoms fatty acids. Compound 6 showed IC50 values of 2.40 ± 0.60, 1.5 ± 0.24, 5.85 ± 1.07 and 5.44 ± 0.24 μM, against HeLa, A-549, PC-3 and LS-180 human cancer cell lines, respectively. Using this information, we performed a quantitative structure-activity relationship (QSAR) of the hybrid molecules and found that the molecular descriptors associated with the antiproliferative activity are: hydrophobic constant associated with substituents (!(!) = 6.5), molecular volume descriptor (!"#!"#$%& ≈ 700 Å!), !!"#", number of rotatable bonds (!"#) and number of 6-membered rings (!"06). Results: The geranic acid and berberine hybrid compound (6) improved the antiproliferative activity shown by natural berberine, even more than the 16- to 18-carbon atoms fatty acids. Compound 6 showed IC50 values of 2.40 ± 0.60, 1.5 ± 0.24, 5.85 ± 1.07 and 5.44 ± 0.24 μM, against HeLa, A-549, PC-3 and LS-180 human cancer cell lines, respectively. Using this information, we performed a quantitative structure-activity relationship (QSAR) of the hybrid molecules and found that the molecular descriptors associated with the antiproliferative activity are: hydrophobic constant associated with substituents (!(!) = 6.5), molecular volume descriptor (!"#!"#$%& ≈ 700 Å!), !!"#", number of rotatable bonds (!"#) and number of 6-membered rings (!"06). Conclusion: The methylendioxy and methoxyl groups in berberine are important for the antiproliferative activity shown by its derivatives. Better results in antiproliferative activity were obtained in compound 6 with the prenyl moiety. The QSAR indicates that the molecular descriptors which associated positively with the antiproliferative activity are: hydrophobic constant associated with substituents (! ! = 6.5), molecular volume descriptor (!"#!"#$%& ≈700 Å3) and !!"#". This research gave the basis for the design and preparation of new, easily afforded molecules derived from berberine and carboxylic acids, with improved antiproliferative activity. Conclusion: The methylendioxy and methoxyl groups in berberine are important for the antiproliferative activity shown by its derivatives. Better results in antiproliferative activity were obtained in compound 6 with the prenyl moiety. The QSAR indicates that the molecular descriptors which associated positively with the antiproliferative activity are: hydrophobic constant associated with substituents (! ! = 6.5), molecular volume descriptor (!"#!"#$%& ≈700 Å3) and !!"#". This research gave the basis for the design and preparation of new, easily afforded molecules derived from berberine and carboxylic acids, with improved antiproliferative activity.

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28

Moreno-Félix, Carolina, Griselda Wilson-Sánchez, Susana-Gabriela Cruz-Ramírez, Carlos Velázquez-Contreras, Maribel Plascencia-Jatomea, Ana Acosta, Lorena Machi-Lara, et al. "Bioactive Lipidic Extracts from Octopus (Paraoctopus limaculatus): Antimutagenicity and Antiproliferative Studies." Evidence-Based Complementary and Alternative Medicine 2013 (2013): 1–12. http://dx.doi.org/10.1155/2013/273582.

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Fractions from an organic extract from fresh octopus (Paraoctopus limaculatus) were studied for biological activities such as antimutagenic and antiproliferative properties usingSalmonellatester strains TA98 and TA100 with metabolic activation (S9) and a cancer cell line (B-cell lymphoma), respectively. A chloroform extract obtained from octopus tentacles was sequentially fractionated using thin layer chromatography (TLC), and each fraction was tested for antimutagenic and antiproliferative activities. Organic extract reduced the number of revertants caused by aflatoxin B1showing a dose-response type of relationship. Sequential TLC fractionation of the active extracts produced several antimutagenic and/or antiproliferative fractions. Based on the results obtained, the isolated fractions obtained from octopus contain compounds with chemoprotective properties that reduce the mutagenicity of AFB1and proliferation of cancer cell lines.

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Benigno, Daniela, Antonella Virgilio, Ivana Bello, Sara La Manna, Valentina Vellecco, Mariarosaria Bucci, Daniela Marasco, Elisabetta Panza, Veronica Esposito, and Aldo Galeone. "Properties and Potential Antiproliferative Activity of Thrombin-Binding Aptamer (TBA) Derivatives with One or Two Additional G-Tetrads." International Journal of Molecular Sciences 23, no. 23 (November 29, 2022): 14921. http://dx.doi.org/10.3390/ijms232314921.

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In this paper, we study the biological properties of two TBA analogs containing one and two extra G-tetrads, namely TBAG3 and TBAG4, respectively, and two further derivatives in which one of the small loops at the bottom (TBAG41S) or the large loop at the top (TBAG4GS) of the TBAG4 structure has been completely modified by replacing all loop residues with abasic site mimics. The therapeutical development of the TBA was hindered by its low thermodynamic and nuclease stability, while its potential as an anticancer/antiproliferative molecule is also affected by the anticoagulant activity, being a side effect in this case. In order to obtain suitable TBA analogs and to explore the involvement of specific aptamer regions in biological activity, the antiproliferative capability against DU 145 and MDAMB 231 cancer cell lines (MTT), the anticoagulant properties (PT), the biological degradability (nuclease stability assay) and nucleolin (NCL) binding ability (SPR) of the above described TBA derivatives have been tested. Interestingly, none of the TBA analogs exhibits an anticoagulant activity, while all of them show antiproliferative properties to the same extent. Furthermore, TBAG4 displays extraordinary nuclease stability and promising antiproliferative properties against breast cancer cells binding NCL efficiently. These results expand the range of G4-structures targeting NCL and the possibility of developing novel anticancer and antiviral drugs.

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Wieczorek, Anna, Andrzej Błauż, Anna Makal, Błażej Rychlik, and Damian Plażuk. "Synthesis and evaluation of biological properties of ferrocenyl–podophyllotoxin conjugates." Dalton Transactions 46, no. 33 (2017): 10847–58. http://dx.doi.org/10.1039/c7dt02107k.

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Lee, Ji Yun, Huarong Yang, Donghwa Kim, Kay Zin Kyaw, Ruoci Hu, Yanhua Fan, and Sang Kook Lee. "Antiproliferative Activity of a New Quinazolin-4(3H)-One Derivative via Targeting Aurora Kinase A in Non-Small Cell Lung Cancer." Pharmaceuticals 15, no. 6 (June 2, 2022): 698. http://dx.doi.org/10.3390/ph15060698.

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Non-small cell lung cancer (NSCLC) is the most common lung cancer subtype. Although chemotherapy and targeted therapy are used for the treatment of patients with NSCLC, the survival rate remains very low. Recent findings suggested that aurora kinase A (AKA), a cell cycle regulator, is a potential target for NSCLC therapy. Previously, we reported that a chemical entity of quinazolin-4(3H)-one represents a new template for AKA inhibitors, with antiproliferative activity against cancer cells. A quinazolin-4(3H)-one derivative was further designed and synthesized in order to improve the pharmacokinetic properties and antiproliferation activity against NSCLC cell lines. The derivative, BIQO-19 (Ethyl 6-(4-oxo-3-(pyrimidin-2-ylmethyl)-3,4-dihydroquinazolin-6-yl)imidazo [1,2-a]pyridine-2-carboxylate), exhibited improved solubility and antiproliferative activity in NSCLC cells, including epidermal growth factor receptor–tyrosine kinase inhibitor (EGFR-TKI)-resistant NSCLC cells. BIQO-19 effectively inhibited the growth of the EGFR-TKI-resistant H1975 NSCLC cells, with the suppression of activated AKA (p-AKA) expression in these cells. The inhibition of AKA by BIQO-19 significantly induced G2/M phase arrest and subsequently evoked apoptosis in H1975 cells. In addition, the combination of gefitinib and BIQO-19 exhibited synergistic antiproliferative activity in NSCLC cells. These findings suggest the potential of BIQO-19 as a novel therapeutic agent for restoring the sensitivity of gefitinib in EGFR-TKI-resistant NSCLC cells.

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Hermane, Jekaterina, Simone Eichner, Lena Mancuso, Benjamin Schröder, Florenz Sasse, Carsten Zeilinger, and Andreas Kirschning. "New geldanamycin derivatives with anti Hsp properties by mutasynthesis." Organic & Biomolecular Chemistry 17, no. 21 (2019): 5269–78. http://dx.doi.org/10.1039/c9ob00892f.

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Four new non hydroquinone derivatives of geldanamycin are prepared by mutasynthesis and their antiproliferative as well as inhibitory properties for human as well as bacterial heatshock proteins are evaluated.

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Ściuk, Anna, Kinga Wątor, Izabela Staroń, Paulina Worsztynowicz, Kinga Pokrywka, Joanna Sliwiak, Marta Kilichowska, et al. "Substrate Affinity Is Not Crucial for Therapeutic L-Asparaginases: Antileukemic Activity of Novel Bacterial Enzymes." Molecules 29, no. 10 (May 11, 2024): 2272. http://dx.doi.org/10.3390/molecules29102272.

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L-asparaginases are used in the treatment of acute lymphoblastic leukemia. The aim of this work was to compare the antiproliferative potential and proapoptotic properties of novel L-asparaginases from different structural classes, viz. EcAIII and KpAIII (class 2), as well as ReAIV and ReAV (class 3). The EcAII (class 1) enzyme served as a reference. The proapoptotic and antiproliferative effects were tested using four human leukemia cell models: MOLT-4, RAJI, THP-1, and HL-60. The antiproliferative assay with the MOLT-4 cell line indicated the inhibitory properties of all tested L-asparaginases. The results from the THP-1 cell models showed a similar antiproliferative effect in the presence of EcAII, EcAIII, and KpAIII. In the case of HL-60 cells, the inhibition of proliferation was observed in the presence of EcAII and KpAIII, whereas the proliferation of RAJI cells was inhibited only by EcAII. The results of the proapoptotic assays showed individual effects of the enzymes toward specific cell lines, suggesting a selective (time-dependent and dose-dependent) action of the tested L-asparaginases. We have, thus, demonstrated that novel L-asparaginases, with a lower substrate affinity than EcAII, also exhibit significant antileukemic properties in vitro, which makes them interesting new drug candidates for the treatment of hematological malignancies. For all enzymes, the kinetic parameters (Km and kcat) and thermal stability (Tm) were determined. Structural and catalytic properties of L-asparaginases from different classes are also summarized.

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Marchidan, Ionuț Georgică, Alina Ortan, Simona Marcu Spinu, Sorin Marius Avramescu, Ionela Avram, Radu Claudiu Fierascu, and Narcisa Babeanu. "Chemical Composition and Biological Properties of New Romanian Lavandula Species." Antioxidants 12, no. 12 (December 16, 2023): 2127. http://dx.doi.org/10.3390/antiox12122127.

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The aims of the present study were to evaluate for the first time the chemical composition and antioxidant, antibacterial, antifungal and antiproliferative potentials of the Romanian George 90 lavender species, as well as parental species, L. angustifolia and L. latifolia. The L. angustifolia, L. latifolia and George 90 essential oils were analyzed by GC-MS/MS and the L. angustifolia, L. latifolia and George 90 hydroalcoholic extracts were analyzed by HPLC-DAD. The antioxidant, antibacterial, antifungal and antiproliferative assays revealed that all the investigated species showed significant activities. The results highlighted the chemical composition and the promising biological potentials of the L. angustifolia, L. latifolia and George 90 lavender species, validating their ethnomedicinal value, which offers potential applications as natural drugs.

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Carullo, Gabriele, Sarah Mazzotta, Francesca Giordano, and Francesca Aiello. "Green Synthesis of New Pyrrolo [1,2-a] quinoxalines as Antiproliferative Agents in GPER-expressing Breast Cancer Cells." Journal of Chemistry 2021 (October 31, 2021): 1–8. http://dx.doi.org/10.1155/2021/5596816.

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4,5-Dihydropyrrolo [1,2-a]quinoxalines are interesting druggable scaffolds, with multifaceted biological properties, including anticancer properties targeting the G protein-coupled estrogen receptor 1 (GPER). In this work, the synthesis and preliminary antiproliferative activity of a small set of new 4,5-dihydropyrrolo[1,2-a]quinoxalines (18-20) and pyrrolo[1,2-a]quinoxalines (21, 22) has been reported, inspired by known antiproliferative agents (G-1, G-15, and G-36). The synthesis of the pyrroloquinoxalinic core was employed following the Pictet–Spengler reaction, using the surfactant p-dodecylbenzene sulphonic acid (p-DBSA), as catalyst. It demonstrated efficiency in the catalysis of the 4-phenylpyrrole [1,2-a] quinoxaline type compound formation in mild solvents such as water, ethanol, and hydroalcoholic solutions. In addition, the reactions proceeded in a short time (between 15 and 120 minutes) at room temperature and with high yields. The in vitro MTT assays showed that the presence of isopropyl groups furnished promising antiproliferative compounds. Although, the acetyl group provided also antiproliferative effects, breaking down its responsibility in the GPER transactivation. Nevertheless, it is possible to conclude that the 4,5-dihydropyrrolo[1,2-a]quinoxalines remain a feasible scaffold to develop anticancer agents against GPER-expressing cells.

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L. Lukov, Georgi, and Tuthill T. "Synergistic antiproliferative effect of mechlorethamine and amyloid beta-peptide on the human lung cancer cell line H441." Cancer Biology & Treatmen 7, no. 1 (August 16, 2021): 1–5. http://dx.doi.org/10.24966/cbt-7546/100017.

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Mechlorethamine (ME) is an antineoplastic agent which has been in clinical use for more than six decades. ME therapy is associated with high toxicity, and it is often in combination with other therapeutics. The use of additional antiproliferative agents could allow the use of ME at lower concentrations, which could lead to comparable therapeutic results, but with lower toxicity. Recent findings have shown that the amyloid β-peptide (Aβ) has antiproliferative properties toward the human cancer cell line, H441 among others. In this study, the cooperative antiproliferative effect of Aβ and ME on the human cell line, H441, isolated from papillary adenocarcinoma lung tissue, was measured. Cells were cultured for 72 hours under standard culturing conditions in growth media containing either Aβ (2 µM), a very low dose of ME (0.2 µM), or both agents combined. We observed a 48% decrease in cell proliferation when Aβ and ME were used simultaneously, compared to 30% and 33% when ME or Aβ, respectively, were used independently. The study demonstrates that the antiproliferative properties of Aβ can augment the anticancer effect of toxic chemotherapeutics such as ME when used at lower doses.

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37

Silyanova, E. A., A. V. Samet, M. N. Semenova, and V. V. Semenov. "Synthesis and antiproliferative properties of 3,4-diarylpyrrole-2-carboxamides." Russian Chemical Bulletin 70, no. 3 (March 2021): 498–509. http://dx.doi.org/10.1007/s11172-021-3115-5.

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Bekisz, Joseph, Samuel Baron, Corey Balinsky, Angel Morrow, and Kathryn C. Zoon. "Antiproliferative Properties of Type I and Type II Interferon." Pharmaceuticals 3, no. 4 (March 30, 2010): 994–1015. http://dx.doi.org/10.3390/ph3040994.

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39

Pokrovskii, VS, EM Treshchalina, NV Andronova, and SM Deev. "Ribonucleases with Antiproliferative Properties: Molecular Biological and Biochemical Characteristics." Clinical oncohematology 9, no. 2 (2016): 130–37. http://dx.doi.org/10.21320/2500-2139-2016-9-2-130-137.

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40

Chi, Chun-Lan, Lu Xu, Jun-Jie Li, Yang Liu, and Bao-Quan Chen. "Synthesis, antiproliferative, and antimicrobial properties of novel phthalimide derivatives." Medicinal Chemistry Research 31, no. 1 (November 23, 2021): 120–31. http://dx.doi.org/10.1007/s00044-021-02823-5.

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41

Benahmed, Fatiha, Elazhari Mehrab, and Omar Kharoubi. "Phytochemical analysis and antiproliferative properties of Pistacia atlantica leaves." Journal of Drug Delivery and Therapeutics 11, no. 6-S (December 15, 2021): 21–25. http://dx.doi.org/10.22270/jddt.v11i6-s.5209.

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The medicinal plants may serve as potential sources for the development of new drugs and more effective anticancer agents for future therapy. Pistacia atlantica (Vahl.) Masters (Anacardiaceae) is an important plant used in traditional medicine practice in Algeria, and North Africa countries. The present study has the objective to estimate the in vitro antiproliferative (on the RD and Hep2 human tumor cell lines using the3-[4,5-dimethylthiazol-2-yl]-2,5-diphenyltetrazolium (MTT) assay) properties of the aqueous extracts of P. atlantica leaves, offering a phytochemical characterization of its aqueous extracts, by spectrophotometry methods. evealed by HPLC, phenolic compounds present among the five different flavonoids identified such as: ((epi)catechin, myricetin, quercetin and kaempferol glycoside derivatives). The MTT assay revealed that the tested extract had a good activity against Hep2 and RD cell lines with median inhibitory concentration (GI50)> 1000 μg/mL against Hep2 and (IC50) = 825,079 μg/mL against RD, (GI 50). The results showed a great bioactive potential for this species with a significant contribution of phenolic compounds, specially the flavonoids which makes it an interesting matrix in the development of novel pharmaceutical formulations. Planned future studies will involve the identification of different extract other than aqueous extract, determination of the mechanisms of action and the bioactive molecule of plant extracts. Keywords: Pistacia atlantica; aqueous extract; antiproliferative; MTT, HPLC.

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Bergeron, Raymond J., James S. McManis, Charles Z. Liu, Yang Feng, William R. Weimar, Gabriel R. Luchetta, Qianhong Wu, Jackqueline Ortiz-Ocasio, and J. R. Timothy Vinson. "Antiproliferative Properties of Polyamine Analogs: A Structure-Activity Study." Journal of Medicinal Chemistry 37, no. 21 (October 1994): 3464–76. http://dx.doi.org/10.1021/jm00047a004.

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Muthna, Darina, Jana Cmielova, Pavel Tomsik, and Martina Rezacova. "Boldine and Related Aporphines: From Antioxidant to Antiproliferative Properties." Natural Product Communications 8, no. 12 (December 2013): 1934578X1300801. http://dx.doi.org/10.1177/1934578x1300801235.

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Plant and folk medicine represent nowadays a source of either new therapeutic substances or substrates for drug synthesis. One such promising group for possible further exploitation is the family of aporphine alkaloids containing boldine and related compounds. In this mini-review we focus on boldine and its newly described effects, which predominantly arise from its antioxidant properties. Moreover, we try to compare its antiproliferative properties with other better known members of the aporphine group.

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44

Torres-Moreno, H., J. C. López-Romero, J. Y. Vázquez-Solorio, C. A. Velázquez-Contreras, A. Garibay-Escobar, R. Díaz-López, and R. E. Robles-Zepeda. "Antioxidant, anti-inflammatory and antiproliferative properties of Ibervillea sonorae." South African Journal of Botany 125 (September 2019): 207–13. http://dx.doi.org/10.1016/j.sajb.2019.07.029.

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Imperatore, Concetta, Mohammadhassan Valadan, Luciana Tartaglione, Marco Persico, Anna Ramunno, Marialuisa Menna, Marcello Casertano, et al. "Exploring the Photodynamic Properties of Two Antiproliferative Benzodiazopyrrole Derivatives." International Journal of Molecular Sciences 21, no. 4 (February 13, 2020): 1246. http://dx.doi.org/10.3390/ijms21041246.

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The identification of molecules whose biological activity can be properly modulated by light is a promising therapeutic approach aimed to improve drug selectivity and efficacy on the molecular target and to limit the side effects compared to traditional drugs. Recently, two photo-switchable diastereomeric benzodiazopyrrole derivatives 1RR and 1RS have been reported as microtubules targeting agents (MTAs) on human colorectal carcinoma p53 null cell line (HCT 116 p53-/-). Their IC50 was enhanced upon Light Emitting Diode (LED) irradiation at 435 nm and was related to their cis form. Here we have investigated the photo-responsive behavior of the acid derivatives of 1RR and 1RS, namely, d1RR and d1RS, in phosphate buffer solutions at different pH. The comparison of the UV spectra, acquired before and after LED irradiation, indicated that the trans→cis conversion of d1RR and d1RS is affected by the degree of ionization. The apparent rate constants were calculated from the kinetic data by means of fast UV spectroscopy and the conformers of the putative ionic species present in solution (pH range: 5.7–8.0) were modelled. Taken together, our experimental and theoretical results suggest that the photo-conversions of trans d1RR/d1RS into the corresponding cis forms and the thermal decay of cis d1RR/d1RS are dependent on the presence of diazonium form of d1RR/d1RS. Finally, a photo-reaction was detected only for d1RR after prolonged LED irradiation in acidic medium, and the resulting product was characterized by means of Liquid Chromatography coupled to High resolution Mass Spectrometry (LC-HRMS) and Nuclear Magnetic Resonance (NMR) spectroscopy.

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Wysokińska, H., L. Światek, and J. Kunert-Radek. "Antiproliferative Properties of Iridoids from Tissue Cultures ofPenstemon serrulatus." Planta Medica 57, S 2 (December 1991): A65—A66. http://dx.doi.org/10.1055/s-2006-960328.

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Shchekotikhin, Andrey E., Vladimir N. Buyanov, and Maria N. Preobrazhenskaya. "Synthesis of 1-(ω-aminoalkyl)naphthoindolediones with antiproliferative properties." Bioorganic & Medicinal Chemistry 12, no. 14 (July 2004): 3923–30. http://dx.doi.org/10.1016/j.bmc.2004.04.042.

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Singh, Ravi P., Marian N. Aziz, Delphine Gout, Walid Fayad, May A. El-Manawaty, and Carl J. Lovely. "Novel thiazolidines: Synthesis, antiproliferative properties and 2D-QSAR studies." Bioorganic & Medicinal Chemistry 27, no. 20 (October 2019): 115047. http://dx.doi.org/10.1016/j.bmc.2019.115047.

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da Silva, Daniel L., Fabiano S. Reis, Dandara R. Muniz, Ana Lúcia T. G. Ruiz, João E. de Carvalho, Adão A. Sabino, Luzia V. Modolo, and Ângelo de Fátima. "Free radical scavenging and antiproliferative properties of Biginelli adducts." Bioorganic & Medicinal Chemistry 20, no. 8 (April 2012): 2645–50. http://dx.doi.org/10.1016/j.bmc.2012.02.036.

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Fernandes, Iva, Filipe Marques, Victor de Freitas, and Nuno Mateus. "Antioxidant and antiproliferative properties of methylated metabolites of anthocyanins." Food Chemistry 141, no. 3 (December 2013): 2923–33. http://dx.doi.org/10.1016/j.foodchem.2013.05.033.

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