2. Academic Validation
  3. Novel chromene-derived selective estrogen receptor modulators useful for alleviating hot flushes and vaginal dryness

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

Affiliation

  • 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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