吲唑并吡唑并嘧啶作为强效 B-Raf 抑制剂具有体内活性。
Indazolylpyrazolopyrimidine as highly potent B-Raf inhibitors with in vivo activity.
机构信息
Pfizer Global Research and Development, 401 N Middletown Road, Pearl River, New York 10965, United States.
出版信息
J Med Chem. 2010 Nov 11;53(21):7874-8. doi: 10.1021/jm1007566.
PMID:20961062
Abstract
Novel indazolylpyrazolo[1,5-a]pyrimidine analogues have been prepared and found to be extremely potent type I B-Raf inhibitors. The lead compound shows good selectivity against a panel of 60 kinases, possesses a desirable pharmacokinetic profile, and demonstrates excellent in vivo antitumor efficacy in B-Raf mutant xenograft models.
摘要
新型吲唑并吡唑并[1,5-a]嘧啶类似物已被制备出来，并被发现是非常有效的 I 型 B-Raf 抑制剂。该先导化合物对 60 种激酶具有良好的选择性，具有理想的药代动力学特征，并在 B-Raf 突变型异种移植模型中表现出优异的体内抗肿瘤疗效。
Zotero 插件