Publications Repository - Gdańsk University of Technology

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.

Authors

• Aneta Pogorzelska,
• Jarosław Sławiński,
• Anna Kawiak,
• Beata Żołnowska,
• prof. dr hab. inż. Jarosław Chojnacki link open in new tab ,
• Grzegorz Stasiłojć,
• Szymon Ulenberg,
• dr Krzysztof Szafrański,
• Tomasz Bączek