Discovery of 6-benzyloxyquinolines as c-Met selective kinase inhibitors

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• 作者：Hiroki Nishii ; Takashi Chiba ; Kenji Morikami ; Takaaki A. Fukami ; Hiroshi Sakamoto ; Kwangseok Ko ; Hiroshi Koyano
• 关键词：6-Benzyloxyquinolines ; c-Met ; Kinase inhibitor
• 刊名：Bioorganic and Medicinal Chemistry Letters
• 出版年：2010
• 出版时间：15 February 2010
• 年：2010
• 卷：20
• 期：4
• 页码：1405-1409
• 全文大小：728 K

文摘

A novel quinoline derivative that selectively inhibits c-Met kinase was identified. The molecular design is based on a result of the analysis of a PF-2341066 (1)/c-Met cocrystal structure (PDB code: 2wgj). The kinase selectivity of the derivatives is discussed from the view point of the sequence homology of the kinases, the key interactions found in X-ray cocrystal structures, and the structure–activity relationship (SAR) obtained in this work.