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First generation 5-vinyl-3-pyridinecarbonitrile PKC theta inhibitors

  作者 Niu, CS; Boschelli, DH; Tumey, LN; Bhagirath, N; Subrath, J; Shim, J; Wang, Y; Wu, BQ; Eid, C; Lee, J; Yang, XK; Brennan, A; Chaudhary, D  
  选自 期刊  Bioorganic & Medicinal Chemistry Letters;  卷期  2009年19-20;  页码  5829-5832  
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[摘要]A series of 5-vinyl-3-pyridinecarbonitriles were synthesized and evaluated as PKC theta inhibitors. The systematic optimization of 4-[(4-methyl-1H-indol-5-yl)amino]-5-[(E)-2-phenylvinyl]-3-pyridinecarbonitrile 3 resulted in the identification of compound 23e as a potent PKC theta inhibitor with good selectivity over PKC delta. (C) 2009 Elsevier Ltd. All rights reserved.

 
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