Novel chromene-derived selective estrogen receptor modulators useful for alleviating hot flushes and vaginal dryness

  • J Med Chem. 2006 Jun 1;49(11):3056-9. doi: 10.1021/jm060353u.
Nareshkumar Jain  1 ,  Ramesh M Kanojia ,  Jiayi Xu ,  Guo Jian-Zhong ,  Emmanuel Pacia ,  Muh-Tsann Lai ,  Fuyong Du ,  Amy Musto ,  George Allan ,  DoWon Hahn ,  Scott Lundeen ,  Zhihua Sui
Affiliations
  • 1. Johnson & Johnson Pharmaceutical Research & Development LLC, 1000 Route 202, Raritan, New Jersey 08869, USA.
PMID: 16722623 DOI: 10.1021/jm060353u
Abstract

A novel SERM (selective Estrogen Receptor modulators), 1-(R), a chromene-derived bisbenzopyran, was discovered to alleviate hot flushes and effectively increase vaginal fluidity in rats. Moreover, 1-(R) was found to have beneficial effects on plasma Cholesterol and bone metabolism while maintaining antiestrogenic activity in the uterus. The biological profile of its enantiomer 1-(S) was also evaluated.

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