Synthesis and Evaluation of [2-(4-Quinolyloxy)phenyl]methanone Derivatives: Novel Selective Inhibitors of Transforming Growth Factor-β Kinase
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- 作者：Toshiyuki Shimizu ; Kaname Kimura ; Teruyuki Sakai ; Kazuki Kawakami ; Tetsuko Miyazaki ; Masayoshi Nakouji ; Akira Ogawa ; Hitomi Ohuchi ; Kiyoshi Shimizu
- 刊名：Journal of Medicinal Chemistry
- 出版年：2008
- 出版时间：June 12, 2008
- 年：2008
- 卷：51
- 期：11
- 页码：3326 - 3329
- 全文大小：190K
- 年卷期：v.51,no.11(June 12, 2008)
- ISSN：1520-4804
文摘
We synthesized and evaluated various [2-(4-quinolyloxy)phenyl]methanone derivatives. These compounds had novel chemical structures that were distinct from those of previously reported inhibitors. Biological data suggested that these compounds inhibited transforming growth factor-β signaling by interacting with the ATP-binding pocket of the transforming growth factor-β type I receptor kinase domain. Here, we report on the synthesis and structure−activity relationships of the compounds in this series.