标题：Design, synthesis, and biological evaluation of 2-(5-methyl-1H-pyrazol-1-yl) acetamide derivatives as androgen receptor antagonists
作者：Dong, Junze; Zhang, Jingya; Li, Zilu; Asnake, Solomon; Zhang, Daoguang; Olsson, Per-Erik; Zhao, Guisen
作者机构：[Dong, Junze; Zhang, Jingya; Li, Zilu; Zhang, Daoguang; Zhao, Guisen] Shandong Univ, Sch Pharmaceut Sci, Dept Med Chem, Key Lab Chem Biol,Minist Educ, 更多
通讯作者地址：[Zhao, GS]Shandong Univ, Sch Pharmaceut Sci, Dept Med Chem, Key Lab Chem Biol,Minist Educ, Jinan 250012, Shandong, Peoples R China.
来源：MEDICINAL CHEMISTRY RESEARCH
关键词：Androgen receptor; Prostate cancer; Antagonists; Pyrazole derivatives
摘要：Androgen receptor (AR) signaling is often activated in prostate cancer (PCa) cells, and blockage of this signaling by AR antagonists is an important strategy in PCa therapy. In this study, we designed and synthesized a series of 2-(5-methyl-1H-pyrazol-1-yl) acetamide derivatives, and evaluated their biological activities. AR luciferase reporter assay revealed compound 6f (59.7%) as a potent AR antagonist. Some compounds in this series showed higher anti-proliferative activity against LNCaP cells than Bicalutamide (IC50=35.0M), especially 6g with IC50 value of 13.6 mu M.