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Discovery and optimization of pyrazoline compounds as B-Raf inhibitors

  作者 Duffey, MO; Adams, R; Blackburn, C; Chau, RW; Chen, S; Galvin, KM; Garcia, K; Gould, AE; Greenspan, PD; Harrison, S; Huang, SC; Kim, MS; Kulkarni, B; Langston, S; Liu, JX; Ma, LT; Menon, S; Nagayoshi, M; Rowland, RS; Vos, TJ; Xu, TL; Yang, JJ; Yu, SX; Zhang, Q  
  选自 期刊  Bioorganic & Medicinal Chemistry Letters;  卷期  2010年20-16;  页码  4800-4804  
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[摘要]The discovery of novel pyrazoline derivatives as B-Raf (V600E) inhibitors is described in this report. Chemical modi. cation of the pyrazoline scaffold led to the development of SAR and identified potent and selective inhibitors of B-Raf (V600E). Determination of the pharmacokinetic properties of selected inhibitors is also reported. (C) 2010 Elsevier Ltd. All rights reserved.

 
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