- Synthesis and evaluation of [2-(4-quinolyloxy)phenyl]methanone derivatives: Novel selective inhibitors of transforming growth factor-β kinase
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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.
- Shimizu, Toshiyuki,Kimura, Kaname,Sakai, Teruyuki,Kawakami, Kazuki,Miyazaki, Tetsuko,Nakouji, Masayoshi,Ogawa, Akira,Ohuchi, Hitomi,Shimizu, Kiyoshi
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- COMPOUND HAVING TGF-BETA INHIBITORY ACTIVITY AND MEDICINAL COMPOSITION CONTAINING THE SAME
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The present invention provides compounds represented by formula (I) and pharmaceutically acceptable salts and solvates thereof: wherein X represents CH or N; Z represents -O-, -NH- or - C(=O)-; R and R' represent a hydrogen atom, hydroxyl, a halogen atom, optionally substituted alkyl, optionally substituted alkenyl optionally substituted alkoxy, amino, aminocarbonyl, or an optionally substituted heterocyclic group; and A represents an optionally substituted specific carbocyclic or heterocyclic group. The compounds according to the present invention have excellent TGFβ inhibitory activity.
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(2008/06/13)
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