Y. Zhu
2015
Citations
0
Influential Citations
0
Citations
Quality indicators
Journal
Chinese Journal of Synthetic Chemistry
Abstract
Two intermediates,N-【3-fluoro-4-【{ 2-[5-( trifluoromethyl)-1H-imidazol-2-yl]oxy】-phenyl】acetamide( 7a) and N-【4-【{ 2-[5-( trifluoromethyl)-1H-imidazol-2-yl]pyridin-4-yl} oxy】-phenyl】acetamide( 7d),were obtained by a six-step reaction from 4-chloropicolinic acid. Six novel imidazole acyl urea derivatives Raf kinase inhibitors( 9a ~ 9f) were synthesized by the reaction of 7a and7 d with substituted benzoyl isothiocyanate,respectively. The structures were characterized by1 H NMR and ESI-MS. The antitumor activities of 9a ~ 9f against human gastric carcinoma cell line( BGC823) were investigated by MTT method. The results showed that 4-chloro-N-【【3-fluoro-4-【{ 2-[5-( trifluoromethyl)-1H-imidazol-2-yl]oxy】pyridin-4-yl} 】-phenyl】carbamothioyl】benzamide( 9c)and N-【【3-fluoro-4-【{ 2-[5-( trifluoromethyl)-1H-imidazol-2-yl]pyridin-4-yl} oxy】-phenyl】carbamothioyl】-3-( pyridin-3-yl) acrylamide( 9d) exhibited similar inhibitory activities to Sorafenib( 70.97%). The inhibitory activities of 9c and 9d were 66. 86% and 63. 60% with dosage of 100 μg,respectively。