Potent, nonsteroidal selective androgen receptor modulators (SARMs) based on 8H-[1,4]oxazino[2,3-f]quinolin-8-ones.
Potent, nonsteroidal selective androgen receptor modulators (SARMs) based on 8H-[1,4]oxazino[2,3-f]quinolin-8-ones.
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基于 8H-[1,4]恶嗪基[2,3-f]喹啉-8-酮的有效非甾体选择性雄激素受体调节剂 (SARM)。
DOI：
10.1016/j.bmcl.2007.07.034
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发表时间：
2007
影响因子：
2.7
通讯作者：
M
中科院分区：
文献类型：
--
作者：
Higuchi,RobertI;Thompson,AnthonyW;Chen,Jyun-Hung;Caferro,ThomasR;Cummings,MarquisL;Deckhut,CharlotteP;Adams,MarkE;Tegley,ChristopherM;Edwards,JamesP;López,FranciscoJ;Kallel,EAdam;Karanewsky,DonaldS;Schrader,WilliamT;M
合成了一系列基于8H-[1，4]恶嗪并[2，3-f]喹啉-8-酮的雄激素受体调节剂，并在雄激素受体转录激活试验中进行了评价。该系列中最有效的类似物在体外表现出个位数纳摩尔的效力。在雄激素作用的体内模型中，化合物18 h在10 mg/kg下表现出维持肌肉重量的完全功效，同时前列腺重量的活性降低。
A series of androgen receptor modulators based on 8H-[1,4]oxazino[2,3-f]quinolin-8-ones was synthesized and evaluated in an androgen receptor transcriptional activation assay. The most potent analogues from the series exhibited single-digit nanomolar potency in vitro. Compound 18h demonstrated full efficacy in the maintenance of muscle weight, at 10mg/kg, with reduced activity in prostate weight in an in vivo model of androgen action.