Synthesis and structure-activity relationship of novel 6-aryl-1,4-dihydrobenzo[d][1,3]oxazine-2-thiones as progesterone receptor modulators leading to the potent and selective nonsteroidal progesterone receptor agonist tanaproget

被引：95

作者：

Fensome, A

Bender, R

Chopra, A

Cohen, J

Collins, MA

Hudak, V

Malakian, K

Lockhead, S

Olland, A

Svenson, K

Terefenko, EA

Unwalla, RJ

Wilhelm, JM

Wolfrom, S

Zhu, Y

Zhang, ZM

Zhang, PW

Winneker, RC

Wrobel, J

机构：

[1] Wyeth Res, Chem & Screening Sci, Collegeville, PA 19426 USA

[2] Wyeth Res, Womens Hlth Res Inst, Collegeville, PA 19426 USA

[3] Wyeth Res, Drug Safety & Metab, Collegeville, PA 19426 USA

来源：

JOURNAL OF MEDICINAL CHEMISTRY | 2005年 / 48卷 / 16期

关键词：

D O I：

10.1021/jm050358b

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

Tanaproget represents a potential first-in-class nonsteroidal PR agonist for contraception with improved safety and side effect profiles versus currently available steroidal oral contraceptives. Additional SAR, biological activity, and structural information from a tanaproget/hPR-LBD (hPR-LBD human progesterone receptor ligand binding domain) cocrystal structure will also be presented.

引用

页码：5092 / 5095

页数：4

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