Design, Synthesis, and in Vitro Evaluation of Novel 3, 7-Disubstituted Coumarin Derivatives as Potent Anticancer Agents

Yubin Wang, Haitao Liu, Peng Lu, Rui Mao, Xiaojian Xue, Chen Fan, Jinxiong She

Research output: Contribution to journalArticle

10 Scopus citations

Abstract

Twenty-seven 3, 7-disubstituted coumarin derivatives were designed, synthesized, and evaluated in vitro as anticancer agents. Most of the compounds showed moderate-to-potent antiproliferative activity against K562 cells. Compounds 7b and 7d were chosen to evaluate the concentration of 50% growth inhibition (GI50) against SN12C, OVCAR, BxPC-3, KATO-III, T24, SNU-1, WiDr, HeLa, K562, and AGS cell lines. The most potent compound 7d was selected for further cell cycle arrest assay in the AGS cell line. The in vitro data indicated that methylation of benzimidazole moiety at the 3-position of coumarin exhibited significant enhancement of anticancer activity. This study should provide important information for further modification and optimization of coumarin derivatives as anticancer agents.

Original languageEnglish (US)
Pages (from-to)637-647
Number of pages11
JournalChemical Biology and Drug Design
Volume86
Issue number4
DOIs
StatePublished - Oct 1 2015
Externally publishedYes

Keywords

  • 3 7-disubstituted
  • Coumarin
  • anticancer activity
  • synthesis

ASJC Scopus subject areas

  • Biochemistry
  • Molecular Medicine
  • Pharmacology
  • Drug Discovery
  • Organic Chemistry

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