一系列5-乙烯基苯磺酰胺-3-吡啶甲腈的合成及蛋白激酶Cθ抑制活性
Synthesis and PKCtheta inhibitory activity of a series of 5-vinyl phenyl sulfonamide-3-pyridinecarbonitriles.
作者信息
Shim Jaechul, Eid Clark, Lee Julie, Liu Erica, Chaudhary Divya, Boschelli Diane H
机构信息
Chemical Sciences, Wyeth Research, Pearl River, NY 10965, USA.
出版信息
Bioorg Med Chem Lett. 2009 Dec 1;19(23):6575-7. doi: 10.1016/j.bmcl.2009.10.031. Epub 2009 Oct 13.
PMID:19854645
Abstract
A series of 5-vinyl phenyl sulfonamide-3-pyridinecarbonitriles were prepared and evaluated as PKCtheta inhibitors. Optimization resulted in the identification of compound 15 with an IC(50) value 0.44 nM for the inhibition of PKCtheta with 150-fold selectivity over PKCdelta.
摘要
制备了一系列5-乙烯基苯磺酰胺-3-吡啶甲腈，并将其作为蛋白激酶Cθ（PKCθ）抑制剂进行评估。通过优化，确定了化合物15，其对PKCθ抑制作用的半数抑制浓度（IC50）值为0.44 nM，对PKCδ的选择性是其150倍。
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