4.7 Article

Benzopyrans are selective estrogen receptor β agonists with novel activity in models of benign prostatic hyperplasia

Journal

JOURNAL OF MEDICINAL CHEMISTRY
Volume 49, Issue 21, Pages 6155-6157

Publisher

AMER CHEMICAL SOC
DOI: 10.1021/jm060491j

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Benzopyran selective estrogen receptor beta agonist-1 (SERBA-1) shows potent, selective binding and agonist function in estrogen receptor beta (ER beta) in vitro assays. X-ray crystal structures of SERBA-1 in ER alpha and beta help explain observed, beta-selectivity of this ligand. SERBA-1 in vivo demonstrates involution of the ventral prostate in CD-1 mice (ER beta effect), while having no effect on gonadal hormone levels (ER alpha effect) at 10 x the efficacious dose, consistent with in vitro properties of this molecule.

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