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Synthesis and evaluation of pyrazolo[1,5-b]pyridazines as selective cyclin dependent kinase inhibitors

  作者 Stevens, KL; Reno, MJ; Alberti, JB; Price, DJ; Kane-Carson, LS; Knick, VB; Shewchuk, LM; Hassell, AM; Veal, JM; Davis, ST; Griffin, RJ; Peel, MR  
  选自 期刊  Bioorganic & Medicinal Chemistry Letters;  卷期  2008年18-21;  页码  5758-5762  
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[摘要]A novel series of pyrazolo[1,5-b]pyridazines have been synthesized and identified as cyclin dependant kinase inhibitors potentially useful for the treatment of solid tumors. Modi. cation of the hinge-binding amine or the C(2)- and C(6)- substitutions on the pyrazolopyridazine core provided potent inhibitors of CDK4 and demonstrated enzyme selectivity against VEGFR-2 and GSK3 beta. (C) 2008 Elsevier Ltd. All rights reserved.

 
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