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

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journal contribution
posted on 01.06.2006, 00:00 by Nareshkumar Jain, Ramesh M. Kanojia, Jiayi Xu, Guo Jian-Zhong, Emmanuel Pacia, Muh-Tsann Lai, Fuyong Du, Amy Musto, George Allan, Hahn, Scott Lundeen, Zhihua Sui
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.