Synthesis and biological evaluation of 2,3,4-triarylbenzopyran derivatives as SERM and therapeutic agent for breast cancer

Bioorg Med Chem. 2009 Oct 1;17(19):6832-40. doi: 10.1016/j.bmc.2009.08.034. Epub 2009 Aug 21.

Abstract

A novel class of 2,3,4-triarylbenzopyrans has been synthesized and were evaluated for their selective estrogen receptor modulation activity and as a therapeutic agent for breast cancer. Among the compounds synthesized, compounds 11a and 12c exhibited 73.91% and 69.24% inhibition as estrogen antagonistic activity, respectively. Compound 12a showed the lowest IC(50) at 6.97 microM against MCF-7 and 11f showed the lowest IC(50) value of 5.6 microM against MDA-MB-231 cell line in spite of their low receptor binding affinity implicating these compounds probably act through ER independent mechanism.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Benzopyrans / chemical synthesis*
  • Benzopyrans / pharmacology
  • Benzopyrans / therapeutic use
  • Breast Neoplasms / drug therapy*
  • Cell Line, Tumor
  • Drug Screening Assays, Antitumor
  • Estrogen Antagonists
  • Female
  • Humans
  • Inhibitory Concentration 50
  • Receptors, Estrogen / metabolism
  • Selective Estrogen Receptor Modulators / chemical synthesis*

Substances

  • Benzopyrans
  • Estrogen Antagonists
  • Receptors, Estrogen
  • Selective Estrogen Receptor Modulators