11β-alkyl-Δ9-19-nortestosterone derivatives:: High-affinity ligands and potent partial agonists of the androgen receptor

被引：9

作者：

Muddana, SS ^{[1
]}

Price, AM ^{[1
]}

MacBride, MM ^{[1
]}

Peterson, BR ^{[1
]}

机构：

[1] Penn State Univ, Dept Chem, University Pk, PA 16802 USA

来源：

JOURNAL OF MEDICINAL CHEMISTRY | 2004年 / 47卷 / 21期

关键词：

D O I：

10.1021/jm0342515

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

We report the synthesis of novel steroidal androgen receptor ligands comprising 11beta-alkyl-Delta(9)-derivatives of 19-nortestosterone. These compounds are structurally related to the antiprogestin, antiglucocorticoid, and antiandrogen drug mifepristone (RU486). Nortestosterone analogues bearing 11beta-octyl and 11beta-decyl side-chains bind tightly to recombinant AR protein (IC50 = 6.6 nM and IC50 = 0.8 nM), block AR dimerization, exhibit activity against LNCaP prostate cancer cells, and comprise partial AR agonists with low antiglucocorticoid activity.

引用

页码：4985 / 4988

页数：4

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