期刊
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
卷 17, 期 3, 页码 784-788出版社
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmcl.2006.10.071
关键词
androgen receptor antagonists; benzimidazoles; prostate weight
The synthesis and in vivo SAR of 5,6-dichloro-benzimidazole derivatives as novel selective androgen receptor antagonists are described. During screening of 2-alkyl benzimidazoles, it was found that a trifluoromethyl group greatly enhances antagonist activity in the prostate. Benzimidazole I is a potent AR antagonist in the rat prostate (ID50 = 0.15 mg/day). (c) 2006 Elsevier Ltd. All rights reserved.
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