Author/Authors :
Toshiyuki Shimizu، نويسنده , , Yasunari Fujiwara، نويسنده , , Tatsushi Osawa، نويسنده , , Teruyuki Sakai، نويسنده , , Kinya Kubo، نويسنده , , Kazuo Kubo، نويسنده , , Tsuyoshi Nishitoba، نويسنده , , Kaname Kimura، نويسنده , , Terufumi Senga، نويسنده , , Hideko Murooka، نويسنده , , Akemi Iwai، نويسنده , , Kayoko Fukushima، نويسنده , , Tetsuya Yoshino، نويسنده , , Atsushi Miwa، نويسنده ,
Abstract :
(6,7-Disubstituted-quinolin-4-yloxy-phenyl)(4-substituted-phenyl)amine derivatives were synthesized and evaluated by a cellular autophosphorylation assay for FGF-R2 in the human scirrhous gastric carcinoma cell line, OCUM-2MD3. We also performed metabolic stability studies showing that substitutions at the 7-position of quinoline affect its biological stability. In this study, we achieved a remarkable improvement in the solubility and metabolic stability of the diphenylamine derivative. The most promising compound 15e showed a significant decrease in tumor volume when orally administered.
Keywords :
Bek. , FGF-R2 , Kinase inhibitor , Quinoline , Anti-proliferation
