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ID: ALA1146677
Journal: Bioorg Med Chem Lett
Title: Orally active anti-proliferation agents: novel diphenylamine derivatives as FGF-R2 autophosphorylation inhibitors.
Authors: Shimizu T, Fujiwara Y, Osawa T, Sakai T, Kubo K, Kubo K, Nishitoba T, Kimura K, Senga T, Murooka H, Iwai A, Fukushima K, Yoshino T, Miwa A.
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.
CiteXplore: 15012985