2-烯基噻吩并[2,3-b]吡啶-5-腈：蛋白激酶Cθ的强效和选择性抑制剂。
2-Alkenylthieno[2,3-b]pyridine-5-carbonitriles: Potent and selective inhibitors of PKCtheta.
作者信息
Nathan Tumey L, Boschelli Diane H, Lee Julie, 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 Aug 1;18(15):4420-3. doi: 10.1016/j.bmcl.2008.06.040. Epub 2008 Jun 18.
PMID:18606543
Abstract
A series of 2-alkenyl thieno[2,3-b]pyridine inhibitors of PKCtheta were synthesized as potential inflammatory modulators. This series led to the discovery of 2-alkenyl amides, which are exceptionally potent and selective inhibitors of PKCtheta. Compound 8 has an IC(50) of 3.8nM against PKCtheta and shows excellent selectivity over a variety of PKC isoforms.
摘要
合成了一系列2-烯基噻吩并[2,3-b]吡啶PKCθ抑制剂，作为潜在的炎症调节剂。该系列化合物导致发现了2-烯基酰胺，它们是PKCθ的异常强效和选择性抑制剂。化合物8对PKCθ的IC(50)为3.8nM，并且对多种PKC同工型显示出优异的选择性。
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