Synthesis and characterization of nonsteroidal glucocorticoid receptor modulators for multiple myeloma.
作者： Andrew R. Hudson , Steven L. Roach , Robert I. Higuchi , Dean P. Phillips , Reid P. Bissonnette
DOI: 10.1021/JM070370Z
关键词:
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 these compounds utilizing a 28 day mouse tumor xenograft model demonstrated efficacy equal dexamethasone the reduction volume.
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