- Synthesis and characterization of nonsteroidal glucocorticoid receptor modulators for multiple myeloma.
Synthesis and characterization of nonsteroidal glucocorticoid receptor modulators for multiple myeloma.
Journal of medicinal chemistry (2007-08-21)
Andrew R Hudson, 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
PMID17705362
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.
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