Multisubstituted indole–acrylonitrile hybrids as potential cytotoxic agents

Bioorganic & Medicinal Chemistry Letters
2014.0

Abstract

A series of multisubstituted indole-acrylonitrile hybrids were designed, synthesized and evaluated for their potential cytotoxic activities. The bio-evaluation results indicated that some of the target compounds (such as 3a, 3f, 3k, 3n) exhibited good to moderate cytotoxic effect on HepG2, BCG-823, BEL-7402, and HL-7702 cell lines. Especially, the compounds 3a and 3k also exhibited high cytotoxic activities (3a, 19.38±3.38 μM; 3k, 15.43±3.54 μM) against the BEL-7402 cell line resistant to Taxol (>25μM) and 5-FU (>500 μM), which might be developed as novel lead scaffold for potential anticancer agents.

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