SYNTHESIS OF NEW COUMARIN DERIVATIVES AND EVALUATION OF THEIR ANTI-CANCER ACTIVITY

Tóm tắt

A fragment based approach has been applied to derive 2-(7-hydroxy-2-oxo-2H-chromen-4-yl)acetic acid 1 into 4 new coumarin derivatives 2a-d through amide bond. The compounds were screening for their anticancer activity using MTT assay on MCF-7 and HepG2 cell lines. The results showed that compounds 2a-c inhibited significantly MCF-7 cells at 40 µM (29-38%) while compound 2d is a strong HepG2 inihibitor with IC₅₀ of 21 µM. Docking studies of the most potent compound 2d suggest its HepG2 antiproliferative activity could be mediated via multikinase inhibition of p38α, VEGFR2 and FGFR-1. Further optimization should lead to more potent compound