Synthesis and identification of novel 11β-aryl-4′,5′-dihydrospiro[estra-4,9-diene-17β,4′-oxazole] analogs with dissociated antiprogesterone activities

被引：15

作者：

Jin, Chunyang

Manikumar, G.

Kepler, John A.

Cook, C. Edgar

Allan, George F.

Kiddoe, Margaret

Bhattacharjee, Sheela

Linton, Olivia

Lundeen, Scott G.

Sui, Zhihua

机构：

[1] RTI Int, Ctr Organ & Med Chem, Res Triangle Pk, NC 27709 USA

[2] Johnson & Johnson Pharmaceut Res & Dev LLC, Drug Discovey, Raritan, NJ 08869 USA

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2007年 / 17卷 / 21期

关键词：

steroidal spiro-oxazole; progesterone receptor; glucocorticoid receptor; antagonist; selective progesterone receptor modulators; PROGESTERONE-RECEPTOR ANTAGONISTS; 11-BETA-ARYL-SUBSTITUTED STEROIDS; CLINICAL-APPLICATIONS; OXA-STEROIDS; MODULATORS; MIFEPRISTONE; EXHIBIT; POTENT; BREAST;

D O I：

10.1016/j.bmcl.2007.08.064

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

A series of novel 11 beta-aryl-4',5'-dihydrospiro[estra-4,9-diene-17 beta,4'-oxazole] analogs have been evaluated for their antagonist hormonal properties using the T47D cell-based alkaline phosphatase assay and the A549 cell-based functional assay. Some of the compounds showed highly potent, and more selective antiprogestational activity against antiglucocorticoid activity than mifepristone (RU 486). (c) 2007 Elsevier Ltd. All rights reserved.

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收藏

页码：5754 / 5757

页数：4

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