| Literature DB >> 15012985 |
Toshiyuki Shimizu1, Yasunari Fujiwara, Tatsushi Osawa, Teruyuki Sakai, Kinya Kubo, Kazuo Kubo, Tsuyoshi Nishitoba, Kaname Kimura, Terufumi Senga, Hideko Murooka, Akemi Iwai, Kayoko Fukushima, Tetsuya Yoshino, Atsushi Miwa.
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.Entities:
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Year: 2004 PMID： 15012985 DOI： 10.1016/j.bmcl.2003.12.019
Source DB: PubMed Journal: Bioorg Med Chem Lett ISSN： 0960-894X Impact factor: 2.823