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
Discovery Research, Ligand Pharmaceuticals, Inc., 10275 Science Center Drive, San Diego, California 92121, USA.
J Med Chem. 2007 Sep 20;50(19):4699-709. doi: 10.1021/jm070370z. Epub 2007 Aug 17.
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.
描述了围绕3'-取代的（Z）-5-（2'-（噻吩基亚甲基））-1,2-二氢-9-羟基-10-甲氧基-2,2,4-三甲基-5H-色烯并[3,4-f]喹啉的构效关系研究。鉴定出了一系列高效且有效的选择性糖皮质激素受体调节剂，其体外活性与地塞米松相当。利用28天小鼠肿瘤异种移植模型对这些化合物进行的体内评估表明，在减少肿瘤体积方面，其疗效与地塞米松相当。
