4.4 Article

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

Journal

CHEMISTRYSELECT
Volume 1, Issue 15, Pages 4638-4644

Publisher

WILEY-V C H VERLAG GMBH
DOI: 10.1002/slct.201600665

Keywords

anticancer; antimicrobial; coumarin-C4-benzimidazole hybrid; 4-formyl coumarin; molecular docking

Funding

  1. UGC-UPE
  2. DST, New Delhi

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New coumarin-benzimidazole hybrids (3a-f) have been synthesized 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 LC50, TGI and GI(50) which show < 10 mg/mL. The synthesized compounds were characterized by IR, NMR, Mass spectral analysis and few of them by single X-ray crystallography analysis.

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