Benzopyrans Are Selective Estrogen Receptor Agonists with Novel Activity in Models of Benign Prostatic Hyperplasia
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- 作者：Bryan H. Norman ; Jeffrey A. Dodge ; Timothy I. Richardson ; Peter S. Borromeo ; Charles W. Lugar ; Scott A. Jones ; Keyue Chen ; Yong Wang ; Gregory L. Durst ; Robert J. Barr ; Chahrzad Montrose-Rafizadeh ; Har
- 刊名：Journal of Medicinal Chemistry
- 出版年：2006
- 出版时间：October 19, 2006
- 年：2006
- 卷：49
- 期：21
- 页码：6155 - 6157
- 全文大小：105K
- 年卷期：v.49,no.21(October 19, 2006)
- ISSN：1520-4804
文摘
Benzopyran selective estrogen receptor beta agonist-1(SERBA-1) shows potent, selective binding and agonist function inestrogen receptor 
hars/beta2.gif" BORDER=0 ALIGN="middle"> (ERhars/beta2.gif" BORDER=0 ALIGN="middle">) in vitro assays. X-ray crystal structures ofSERBA-1 in ERhars/alpha.gif" BORDER=0> and hars/beta2.gif" BORDER=0 ALIGN="middle"> help explain observed hars/beta2.gif" BORDER=0 ALIGN="middle">-selectivity of thisligand. SERBA-1 in vivo demonstrates involution of the ventral prostatein CD-1 mice (ERhars/beta2.gif" BORDER=0 ALIGN="middle"> effect), while having no effect on gonadal hormonelevels (ERhars/alpha.gif" BORDER=0> effect) at 10× the efficacious dose, consistent with in vitroproperties of this molecule.
hars/beta2.gif" BORDER=0 ALIGN="middle"> (ERhars/beta2.gif" BORDER=0 ALIGN="middle">) in vitro assays. X-ray crystal structures ofSERBA-1 in ERhars/alpha.gif" BORDER=0> and hars/beta2.gif" BORDER=0 ALIGN="middle"> help explain observed hars/beta2.gif" BORDER=0 ALIGN="middle">-selectivity of thisligand. SERBA-1 in vivo demonstrates involution of the ventral prostatein CD-1 mice (ERhars/beta2.gif" BORDER=0 ALIGN="middle"> effect), while having no effect on gonadal hormonelevels (ERhars/alpha.gif" BORDER=0> effect) at 10× the efficacious dose, consistent with in vitroproperties of this molecule.