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Triazine and pyrimidine based ROCK inhibitors with efficacy in spontaneous hypertensive rat model

  作者 Ho, KK; Beasley, JR; Belanger, L; Black, D; Chan, JH; Dunn, D; Hu, B; Klon, A; Kultgen, SG; Ohlmeyer, M; Parlato, SM; Ray, PC; Pham, Q; Rong, YJ; Roughton, AL; Walker, TL; Wright, J; Xu, K; Xu, Y; Zhang, LM; Webb, M  
  选自 期刊  Bioorganic & Medicinal Chemistry Letters;  卷期  2009年19-21;  页码  6027-6031  
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[摘要]The pro. le of a series of triazine and pyrimidine based ROCK inhibitors is described. An initial binding mode was established based on a homology model and the proposed interactions are consistent with the observed SAR. Compounds from the series are potent in a cell migration assay and possess a favorable kinase selectivity. In vivo activity was demonstrated for compound 1A in a spontaneous hypertensive rat model. (C) 2009 Published by Elsevier Ltd.

 
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