Synthesis, molecular structure, and metabolic stability of new series of N' -(2-alkylthio-4-chloro-5-methylbenzenesulfonyl)-1-(5-phenyl-1 H -pyrazol-1-yl)amidine as potential anti-cancer agents - Publikacja - MOST Wiedzy

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Synthesis, molecular structure, and metabolic stability of new series of N' -(2-alkylthio-4-chloro-5-methylbenzenesulfonyl)-1-(5-phenyl-1 H -pyrazol-1-yl)amidine as potential anti-cancer agents

Abstrakt

A series of new N'-(2-alkylthio-4-chloro-5-methylbenzenesulfonyl)-1-(5-phenyl-1H-pyrazol-1-yl)amidine derivatives have been synthesized and evaluated in vitro by MTT assays for their antiproliferative activity against cell lines of colon cancer HCT-116, cervical cancer HeLa and breast cancer MCF-7. The studied compounds display selective activity mainly against HCT-116 and HeLa cells. Thus, five compounds show selective cytotoxic effect against HCT-116 (IC50 = 3-10 uM) and HeLa (IC50 = 7 uM). Importantly, the noticed values of IC50 for four compounds are almost 4-fold lower for HeLa than nonmalignant HaCaT cells. More-in-depth biological research revealed that the treatment of HCT-116 and HeLa with active compound resulted in increased numbers of cells in sub-G1 phase in a time dependent manner, while non-active derivative does not influence cell cycle. Metabolic stability assays using liver microsomes and NADPH provide important information on compounds susceptibility to phase 1 biotransformation reactions.

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Aneta Pogorzelska, Jarosław Sławiński, Anna Kawiak, Beata Żołnowska, Jarosław Chojnacki, Grzegorz Stasiłojć, Szymon Ulenberg, Krzysztof Szafrański, Tomasz Bączek. (2018). Synthesis, molecular structure, and metabolic stability of new series of N' -(2-alkylthio-4-chloro-5-methylbenzenesulfonyl)-1-(5-phenyl-1 H -pyrazol-1-yl)amidine as potential anti-cancer agents, 155, 670-680. https://doi.org/10.1016/j.ejmech.2018.06.032

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Informacje szczegółowe

Kategoria:
Publikacja w czasopiśmie
Typ:
artykuł w czasopiśmie wyróżnionym w JCR
Opublikowano w:
EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY nr 155, strony 670 - 680,
ISSN: 0223-5234
Język:
angielski
Rok wydania:
2018
Opis bibliograficzny:
Pogorzelska A., Sławiński J., Kawiak A., Żołnowska B., Chojnacki J., Stasiłojć G., Ulenberg S., Szafrański K., Bączek T.: Synthesis, molecular structure, and metabolic stability of new series of N' -(2-alkylthio-4-chloro-5-methylbenzenesulfonyl)-1-(5-phenyl-1 H -pyrazol-1-yl)amidine as potential anti-cancer agents// EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY. -Vol. 155, (2018), s.670-680

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