当前位置： SCI文献检索 > JOURNAL OF MEDICINAL CHEMISTRY期刊下所有文献 > Design, synthesis, and biological evaluation of 16-substituted 4-azasteroids as tissue-selective androgen receptor modulators (SARMs).

Design, synthesis, and biological evaluation of 16-substituted 4-azasteroids as tissue-selective androgen receptor modulators (SARMs).

Abstract：

:A novel series of 16-substituted-4-azasteroids has been identified as potential tissue-selective androgen receptor modulators. These ligands display potent hAR binding and agonist activity, low virilizing potential, and good pharmacokinetic profiles in dogs. On the basis of its in vitro profile, 21 was evaluated in the OVX and ORX rat models and exhibited an osteoanabolic, tissue-selective profile.

journal_name

J Med Chem

journal_title

Journal of medicinal chemistry

authors

Mitchell HJ,Dankulich WP,Hartman GD,Prueksaritanont T,Schmidt A,Vogel RL,Bai C,McElwee-Witmer S,Zhang HZ,Chen F,Leu CT,Kimmel DB,Ray WJ,Nantermet P,Gentile MA,Duggan ME,Meissner RS

doi

10.1021/jm900880r

subject

Has Abstract

pub_date

2009-08-13 00:00:00

pages

4578-81

issue

15

eissn

0022-2623

issn

1520-4804

journal_volume

52

pub_type

杂志文章

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