2-Amino-4-(aminomethyl)thiazole-based derivatives as potential antitumor agents: design,synthesis, cytotoxicity and apoptosis inducing activities |
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| Institution: | 1. School of Pharmaceutical Sciences, Health Science Center, Shenzhen University, 518060 Shenzhen, China;2. Institute for Inheritance-Based Innovation of Chinese Medicine, Marshall Laboratory of Biomedical Engineering, School of Pharmaceutical Sciences, Health Science Center, Shenzhen University, 518060 Shenzhen, China |
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| Abstract: | Novel 2-amino-4-(aminomethyl)thiazole derivatives were designed and synthesized by a facile method including the Hantzsch construction of thiazole core followed by amidation and nucleophilic substitution steps. Bioassay results showed that 4-(tert-butyl)-N-4-(piperazin-1-ylmethyl)thiazol-2-yl]-benzamide and 4-(tert-butyl)-N-{4-(4-piperidinopiperidin-1-yl)methyl]thiazol-2-yl}benzamide possessed similar activities compared with 5-fluorouracil. The 4-piperidino-piperidin-1-yl-containing derivative also suppressed proliferation of cultured tumor cells by inducing apoptosis. |
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| Keywords: | thiazole derivatives antitumor drug design Hantzsch reaction amidation structure–activity relationship apoptosis |
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