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SYNTHESIS AND ANTIPROLIFERATIVE ACTIVITY STUDY OF NOVEL COUMARIN DERIVATIVES

作者:ZHANG; Keping; WEN; Kai; LIU; Zunfeng;...synthesiscoumarinantiproliferativeactivitytargetinvitro

摘要:A series of coumarin derivatives(A01-A13) have been designed and synthesized, and their biological activities were evaluated in vitro in 5 different cell lines: Liver hepatocellular cells(HepG2), breast cancer cells(MCF-7), human malignant melanoma cells(A375), human colonic carcinoma(HT-29) and non-small cell lung cancer cells(A549). Furthermore, A05 was screened in kinase sets and the results showed that the possible targets of it were MST3/STK24 and TNIK. Compounds A01 and A05 displayed the most potent antiproliferative activities in vitro, which suggested that the picolinamide moiety was important for antiproliferative activities. Compound A05 was screened against a set of kinases and the results indicated the kinases MST3/STK24 and TNIK as possible targets.

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