Design and synthesis of isoquinolines and benzimidazoles as RAF kinase inhibitors

…, L Burgdorf, D Finsinger, F Stieber, C Sirrenberg…

文献索引：Buchstaller, Hans-Peter; Burgdorf, Lars; Finsinger, Dirk; Stieber, Frank; Sirrenberg, Christian; Amendt, Christiane; Grell, Matthias; Zenke, Frank; Krier, Mireille Bioorganic and Medicinal Chemistry Letters, 2011 , vol. 21, # 8 p. 2264 - 2269

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被引用次数: 11

摘要

RAF kinase plays a critical role in the RAF–MEK–ERK signaling pathway and inhibitors of RAF could be of use for the treatment of various cancer types. We have designed potent RAF-1 inhibitors bearing novel bicyclic heterocycles as key structural elements for the interaction with the hinge region. In both series exploration of the SAR was focussed on the substitution of the phenyl ring, which binds to the induced fit pocket. Overall, it was ...