Design, Synthesis and Structure-Activity Relationship Study of Coumarin Benzimidazole Hybrid as Potent Antibacterial and Anticancer Agents

摘要

New coumarin-benzimidazole hybrids (3a–f) have been synthe- sized from 4-formylcoumarins and a series of N-sulphonation (4a-f) and N-methylation (5a-f) compounds were obtained from compounds (3a–f). All the synthesized compounds have exhibited good antimicrobial activity. Docking studies provide valuable insights to potential binding modes of inhibitors. Anti cancer activity of compound 4a and 4c have shown excellent activity against HeLa cell line. Whereas compound 4a and 4d exhibited higher activity against HT 29 cell lines. We calculated the LC_(50), TGI and GI(50) which show < 10 mg/mL. The synthe- sized compounds were characterized by IR, NMR, Mass spectral analysis and few of them by single X-ray crystallography analy- sis.