2. Academic Validation
  3. Synthesis and evaluation of [2-(4-quinolyloxy)phenyl]methanone derivatives: novel selective inhibitors of transforming growth factor-beta kinase

Synthesis and evaluation of [2-(4-quinolyloxy)phenyl]methanone derivatives: novel selective inhibitors of transforming growth factor-beta kinase

  • J Med Chem. 2008 Jun 12;51(11):3326-9. doi: 10.1021/jm701626z.
Toshiyuki Shimizu 1,  Kaname Kimura,  Teruyuki Sakai,  Kazuki Kawakami,  Tetsuko Miyazaki,  Masayoshi Nakouji,  Akira Ogawa,  Hitomi Ohuchi,  Kiyoshi Shimizu
Affiliations

Affiliation

  • 1 KIRIN Pharma Co Ltd, Shibuya, Tokyo, Japan. tshimizu@kirin.co.jp
PMID: 18479116 DOI: 10.1021/jm701626z
Abstract

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-beta signaling by interacting with the ATP-binding pocket of the transforming growth factor-beta type I receptor kinase domain. Here, we report on the synthesis and structure-activity relationships of the compounds in this series.

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