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Synthesis and Biological Evaluation of Novel Anthranilamide Derivatives as Anticancer Agents

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A new series of anthranilamide  derivatives were synthesized and evaluated for their  antiproliferative activities against human colon  carcinoma cell lines (HCT 116) and human breast  adenocarcinoma cell lines (MDA-MB-231) in vitro.  The bioassay results indicated that compounds  7a-7d, 11a, and 11b with flexible linkers showed  promising antiproliferative activity against both cell  lines. Among the compounds synthesized, 7c showed  the most significant antiproliferative activity. Flow  cytometric analysis indicated that 7c inhibited HCT  116 and MDA-MB-231 cell growth by inducing  apoptosis in a dose-dependent manner and suppressed  HCT 116 cell proliferation by G1 and S phase arrest.  Compound 7c may serve as a lead candidate in the  development of novel anticancer agents.

This article was published online in Drug Discoveries and Therapeutics and is free to access.