Synthesis and characterization of nonsteroidal glucocorticoid receptor modulators for multiple myeloma

J Med Chem. 2007 Sep 20;50(19):4699-709. doi: 10.1021/jm070370z.

Andrew R Hudson ¹, Steven L Roach, Robert I Higuchi, Dean P Phillips, Reid P Bissonnette, William W Lamph, Jean Yen, Yongkai Li, Mark E Adams, Lino J Valdez, Angie Vassar, Catalina Cuervo, E Adam Kallel, Catherine J Gharbaoui, Dale E Mais, Jeffrey N Miner, Keith B Marschke, Deepa Rungta, Andrés Negro-Vilar, Lin Zhi

Affiliations

Affiliation

1 Discovery Research, Ligand Pharmaceuticals, Inc., 10275 Science Center Drive, San Diego, California 92121, USA. ahudson@ligand.com

PMID: 17705362 DOI: 10.1021/jm070370z

Abstract

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.

Name
Email *

	Sorry, but the email address you supplied was invalid.