咪唑吡啶
化学
蛋白激酶B
脚手架
激酶
结构-活动关系
药理学
磷酸化
生物化学
体外
立体化学
生物
医学
生物医学工程
作者
Meagan B. Rouse,Mark A. Seefeld,Jack D. Leber,Kenneth C. McNulty,Lihui Sun,William H. Miller,ShuYun Zhang,Elisabeth A. Minthorn,N.O. Concha,Anthony E. Choudhry,Michael D. Schaber,Dirk A. Heerding
标识
DOI:10.1016/j.bmcl.2009.01.002
摘要
AKT inhibitors containing an imidazopyridine aminofurazan scaffold have been optimized. We have previously disclosed identification of the AKT inhibitor GSK690693, which has been evaluated in clinical trials in cancer patients. Herein we describe recent efforts focusing on investigating a distinct region of this scaffold that have afforded compounds (30 and 32) with comparable activity profiles to that of GSK690693.
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