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Synthesis and Evaluation of [2-(4-Quinolyloxy)phenyl]methanone Derivatives: Novel Selective Inhibitors of Transforming Growth Factor-b Kinase.

  作者 Shimizu, Toshiyuki;Kimura, Kaname;Sakai, Teruyuki;Kawakami, Kazuki;Miyazaki, Tetsuko;Nakouji, Masayoshi;Ogawa, Akira;Ohuchi, Hitomi;Shimizu, Kiyoshi;  
  选自 期刊  Journal of Medicinal Chemistry;  卷期  2008年51-11;  页码  3326-3329  
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[摘要]We synthesized and evaluated various [2-(4-quinolyloxy)phenyl]methanone derivs., e.g. I (R = Ph, R1 = H, Me, Br, MeO; R = Me, R1 = H, F, Me, MeO). These compds. had novel chem. structures that were distinct from those of previously reported inhibitors. Biol. data suggested that these compds. inhibited transforming growth factor-b signaling by interacting with the ATP-binding pocket of the transforming growth factor-b type I receptor kinase domain. Here, we report on the synthesis and structure-activity relationships of the compds. in this series.

 
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