Novel Chromene-Derived Selective Estrogen Receptor Modulators Useful for Alleviating Hot Flushes and Vaginal Dryness

Journal of Medicinal Chemistry
2006.0

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.

Knowledge Graph

Similar Paper

Novel Chromene-Derived Selective Estrogen Receptor Modulators Useful for Alleviating Hot Flushes and Vaginal Dryness
Journal of Medicinal Chemistry 2006.0
Identification and Structure−Activity Relationships of Chromene-Derived Selective Estrogen Receptor Modulators for Treatment of Postmenopausal Symptoms
Journal of Medicinal Chemistry 2009.0
Estrogen receptor ligands. Part 10: Chromanes: old scaffolds for new SERAMs
Bioorganic & Medicinal Chemistry Letters 2005.0
Discovery and Synthesis of [6-Hydroxy-3-[4-[2-(1-piperidinyl)ethoxy]phenoxy]- 2-(4-hydroxyphenyl)]benzo[b]thiophene:  A Novel, Highly Potent, Selective Estrogen Receptor Modulator
Journal of Medicinal Chemistry 1997.0
Synthesis and Pharmacology of Conformationally Restricted Raloxifene Analogues:  Highly Potent Selective Estrogen Receptor Modulators
Journal of Medicinal Chemistry 1998.0
Lead identification of a potent benzopyranone selective estrogen receptor modulator
Bioorganic & Medicinal Chemistry Letters 2004.0
2-Phenylspiroindenes: a novel class of selective estrogen receptor modulators (SERMs)
Bioorganic & Medicinal Chemistry Letters 2003.0
Benzopyrans Are Selective Estrogen Receptor β Agonists with Novel Activity in Models of Benign Prostatic Hyperplasia
Journal of Medicinal Chemistry 2006.0
Synthesis and pharmacology of 2-alkyl raloxifene analogs
Bioorganic & Medicinal Chemistry Letters 1996.0
Synthesis and biological evaluation of novel thio-substituted chromanes as high-affinity partial agonists for the estrogen receptor
Bioorganic & Medicinal Chemistry Letters 2002.0