Synthesis and characterization of nonsteroidal glucocorticoid receptor modulators for multiple myeloma

被引：33

作者：

Hudson, Andrew R. ^{[1
]}

Roach, Steven L. ^{[1
]}

Higuchi, Robert I. ^{[1
]}

Phillips, Dean P. ^{[1
]}

Bissonnette, Reid P. ^{[1
]}

Lamph, William W. ^{[1
]}

Yen, Jean ^{[1
]}

Li, Yongkai ^{[1
]}

Adams, Mark E. ^{[1
]}

Valdez, Lino J. ^{[1
]}

Vassar, Angie ^{[1
]}

Cuervo, Catalina ^{[1
]}

Kallel, E. Adam ^{[1
]}

Gharbaoui, Catherine J. ^{[1
]}

Mais, Dale E. ^{[1
]}

Miner, Jeffrey N. ^{[1
]}

Marschke, Keith B. ^{[1
]}

Rungta, Deepa ^{[1
]}

Negro-Vilar, Andrs ^{[1
]}

Zhi, Lin ^{[1
]}

机构：

[1] Ligand Pharmaceut Inc, Discovery Res, San Diego, CA 92121 USA

来源：

JOURNAL OF MEDICINAL CHEMISTRY | 2007年 / 50卷 / 19期

关键词：

D O I：

10.1021/jm070370z

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

Structure-activity relationship studies centered around 3 '-substituted (Z)-5-(2 '-(thienylmethylidene))1,2-dihydro-9-hydroxy-10-methoxy-2,2,4-trimethyl-5H-chromeno[3,4-f]quinolines are described. A series of highly potent and efficacious selective glucocorticoid receptor modulators were identified with in vitro activity comparable to dexamethasone. In vivo evaluation of these compounds utilizing a 28 day mouse tumor xenograft model demonstrated efficacy equal to dexamethasone in the reduction of tumor volume.

引用

页码：4699 / 4709

页数：11

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