Synthesis and characterization of nonsteroidal glucocorticoid receptor modulators for multiple myeloma |
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Authors: | Hudson Andrew R Roach Steven L Higuchi Robert I Phillips Dean P Bissonnette Reid P Lamph William W Yen Jean Li Yongkai Adams Mark E Valdez Lino J Vassar Angie Cuervo Catalina Kallel E Adam Gharbaoui Catherine J Mais Dale E Miner Jeffrey N Marschke Keith B Rungta Deepa Negro-Vilar Andrés Zhi Lin |
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Affiliation: | Discovery Research, Ligand Pharmaceuticals, Inc., 10275 Science Center Drive, San Diego, California 92121, USA. ahudson@ligand.com |
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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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