Synthesis and Cytotoxicity Screening of Some Synthesized Coumarin and Aza-Coumarin Derivatives as Anticancer Agents

摘要

A series of coumarin and aza-coumarin derivatives (II-IX) were synthesized and identified using IR, H-1 NMR, and C-13 NMR spectral data. All the synthesized compounds were assessed for their in vitro antiproliferative activity against Hepatocellular carcinoma (HepG2 cell line), and breast cancer (MCF-7 cell line). In vitro results showed that compounds (III) and (IX) were the most effective compounds against MCF-7 cell line and compound (IV) was the most effective compound against HepG2. Further in vitro study of compounds (III and IX). Compound (III) arrested cell cycle at G2/M phase and induction of apoptosis at pre-G1 phase while compound (IX) arrested cell cycle at G1/S phase. The most potent compounds (III and IX) showed good inhibitory activity against topoisomerase II enzyme. Also, compounds (III and IX) have induced apoptosis at the early and late apoptotic levels.