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Design, synthesis and study of anti-tumor activity of thiazolinone urea derivatives bearing aryloxypyridinone fragments / 药学学报
Yao Xue Xue Bao ; (12): 1696-1704, 2018.
Article en Zh | WPRIM | ID: wpr-780049
Biblioteca responsable: WPRO
ABSTRACT
Taking cabozantinib as leading compound, 13 novel small molecular c-Met inhibitors were designed and synthesized based on the obtained structure-activity relationships (SARs) of c-Met inhibitors. The structures of compounds were confirmed by 1H NMR, 13C NMR and HR-MS. In vitro anti-tumor activity was evaluated by MTT method, and the mechanism was preliminarily disclosed by real-time dynamic living cell imaging and flow cytometry analysis. The results indicated that most of compounds showed good inhibition activity against human non-small-cell carcinoma cell A549 and human colorectal cancer cell HT-29 which was superior to cabozantinb. Compounds showed excellent cytotoxity and anti-proliferative activity against HT-29, and promoted cell apoptosis.
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Texto completo: 1 Índice: WPRIM Idioma: Zh Revista: Yao Xue Xue Bao Año: 2018 Tipo del documento: Article
Texto completo: 1 Índice: WPRIM Idioma: Zh Revista: Yao Xue Xue Bao Año: 2018 Tipo del documento: Article