一系列4-（吲哚-5-基氨基）噻吩并[2,3-b]吡啶-5-腈的合成及蛋白激酶Cθ抑制活性
Synthesis and PKCtheta inhibitory activity of a series of 4-(indol-5-ylamino)thieno[2,3-b]pyridine-5-carbonitriles.
作者信息
Boschelli Diane H, Wu Biqi, Barrios Sosa Ana Carolina, Chen Joan, Asselin Magda, Cole Derek C, Lee Julie, Yang Xiaoke, Chaudhary Divya
机构信息
Wyeth Research, Chemical and Screening Sciences, 401 N. Middletown Road, Pearl River, NY 10965, USA.
出版信息
Bioorg Med Chem Lett. 2008 May 1;18(9):2850-3. doi: 10.1016/j.bmcl.2008.03.077. Epub 2008 Apr 8.
PMID:18434148
Abstract
The thieno[2,3-b]pyridine-5-carbonitrile with a 5-indolylamine at C-4 and a phenyl group at C-2 had a moderate activity against PKCtheta. Optimization of the groups at C-4 and C-2 led to analog 29, which has an IC(50) value of 7.5nM for the inhibition of PKCtheta.
摘要
在C-4位带有5-吲哚胺且在C-2位带有苯基的噻吩并[2,3-b]吡啶-5-腈对蛋白激酶Cθ（PKCθ）具有中等活性。对C-4位和C-2位的基团进行优化得到类似物29，其对PKCθ抑制作用的半数抑制浓度（IC50）值为7.5纳摩尔。
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