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

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Jain N, Kanojia RM, Xu J, Jian-Zhong G, Pacia E, Lai MT, Du F, Musto A, Allan G, Hahn D, Lundeen S, Sui Z

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.

PubMed ID

16722623 [ View in PubMed

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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.

DrugBank Data that Cites this Article

Binding Properties

Drug	Target	Property	Measurement	pH	Temperature (°C)
Ethinylestradiol	Estrogen receptor alpha	IC 50 (nM)	2	N/A	N/A	Details
Raloxifene	Estrogen receptor alpha	IC 50 (nM)	1.8	N/A	N/A	Details
Raloxifene	Estrogen receptor beta	IC 50 (nM)	8.2	N/A	N/A	Details