Biological evaluation and SAR analysis of O-methylated analogs of quercetin as inhibitors of cancer cell proliferation

Drug Dev Res. 2014 Nov;75(7):455-62. doi: 10.1002/ddr.21181. Epub 2014 Jun 27.

Abstract

Using a high-throughout screening approach, the anticancer activities of 16 O-methylated (OMe) analogs of quercetin were assessed. The structure-activity relationships showed that OMe moieties at the 4' and/or 7 positions were important for maintaining inhibitory activities against the 16 cancer cell lines. Furthermore, when the OH groups at the 3' and 4' positions were both replaced by OMe moieties, anticancer activity was enhanced.

Keywords: analog; anticancer; methylation; quercetin; structure-activity relationship.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Antineoplastic Agents / chemical synthesis
  • Antineoplastic Agents / chemistry
  • Antineoplastic Agents / pharmacology*
  • Cell Line, Tumor
  • Cell Proliferation / drug effects
  • Drug Screening Assays, Antitumor
  • Humans
  • Methylation
  • Molecular Structure
  • Neoplasms / pathology*
  • Quercetin / analogs & derivatives*
  • Quercetin / chemistry
  • Quercetin / pharmacology*
  • Structure-Activity Relationship

Substances

  • Antineoplastic Agents
  • Quercetin