Ng Raymond A, Guan Jihua, Alford Vernon C, Lanter James C, Allan George F, Sbriscia Tifanie, Lundeen Scott G, Sui Zhihua
Johnson & Johnson Pharmaceutical Research and Development, LLC, Drug Discovery, 665 Stockton Drive, Exton, PA 19341, USA.
Bioorg Med Chem Lett. 2007 Feb 15;17(4):955-8. doi: 10.1016/j.bmcl.2006.11.047. Epub 2006 Nov 18.
The synthesis and in vivo SAR of N-benzyl, N-aceto, and N-ethylene ether derivatives of 2-(2,2,2-trifluoroethyl)-5,6-dichloro-benzimidazole as novel androgen receptor antagonists are described. SAR studies led to the discovery of 4-bromo-benzyl benzimidazole 17 as a more potent androgen receptor antagonist in the rat prostate (ID(50)=0.13mg/day), compared with bicalutamide (ID(50)=0.23mg/day).
本文描述了2-(2,2,2-三氟乙基)-5,6-二氯苯并咪唑的N-苄基、N-乙酰基和N-乙烯基醚衍生物作为新型雄激素受体拮抗剂的合成及其体内构效关系。构效关系研究发现，与比卡鲁胺（半数抑制剂量（ID(50)）=0.23mg/天）相比，4-溴苄基苯并咪唑17在大鼠前列腺中是一种更有效的雄激素受体拮抗剂（ID(50)=0.13mg/天）。
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