Synthesis, Anticancer and Antibacterial Activities of Novel 2-Amino-4-phenylthiazole Derivatives Containing Amide Moiety

A series of novel 2-amino-4-phenylthiazole derivatives containing amide moiety were designed and synthesized based on the structural features of sorafenib. The structures of synthesized compounds were characterized by H-1 NMR, C-13 NMR and HRMS. Both the anticancer and antibacterial activities of all the target compounds were evaluated. Most of the compounds showed potent activities, especially N-(3-(2-acetamidothiazol-4-yl) phenyl)-3-fluorobenzamide (4n) exhibited a remarkable antitumor effect against human colon cancer cell line (HT29) and human lung epithelial cells (A549) cells with IC50 values of 6.31 and 7.98 mu mol circle L-1, respectively. Further mechanistic study revealed that 4n can influence the Raf/MEK/ ERK pathway. In addition, N-(3-(2-acetamidothiazol-4-yl) phenyl)-3,4-dichlorobenzamide (4h), N-(3-(2-acetamidothiazol-4-yl) phenyl)-3-chlorobenzamide (4i) and N-(3-(2-acetamidothiazol-4-yl) phenyl)-2,4-dichlorobenzamide (4o) exhibit moderate antibacterial activity against the tested bacteria.