Novel flufenamic acid analogues as inhibitors of androgen receptor mediated transcription

ACS Chem Biol. 2009 Oct 16;4(10):834-43. doi: 10.1021/cb900143a.


The androgen receptor (AR), which mediates the signals of androgens, plays a crucial role in prostate-related diseases. Although widely used, currently marketed anti-androgenic drugs have significant side effects. Several studies have revealed that non-steroidal anti-inflammatory drugs, such as flufenamic acid, block AR transcriptional activity. Herein we describe the development of small molecule analogues of flufenamic acid that antagonize AR. This novel class of AR inhibitors binds to the hormone binding site, blocks AR transcription activity, and acts on AR target genes.

Publication types

  • Research Support, N.I.H., Extramural
  • Research Support, Non-U.S. Gov't
  • Research Support, U.S. Gov't, Non-P.H.S.

MeSH terms

  • Androgen Receptor Antagonists*
  • Antineoplastic Agents / chemistry*
  • Antineoplastic Agents / therapeutic use*
  • Antineoplastic Agents, Hormonal
  • Cell Line, Tumor
  • Flufenamic Acid / analogs & derivatives*
  • Flufenamic Acid / therapeutic use*
  • Gene Expression Regulation, Neoplastic / drug effects
  • Humans
  • Male
  • Prostatic Neoplasms / drug therapy
  • Receptors, Androgen / metabolism
  • Structure-Activity Relationship
  • Tacrolimus Binding Proteins / genetics
  • Transcriptional Activation / drug effects*


  • Androgen Receptor Antagonists
  • Antineoplastic Agents
  • Antineoplastic Agents, Hormonal
  • Receptors, Androgen
  • Flufenamic Acid
  • Tacrolimus Binding Proteins
  • tacrolimus binding protein 5