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.

新型 2-amino-4-(aminomethyl)thiazole 衍生物是通过一种简便的方法设计和合成的，包括噻唑核心的 Hantzsch 构造，然后是酰胺化和亲核取代步骤。生物测定结果表明，4-( tert -butyl)- N -[4-(piperazin-1-ylmethyl)thiazol-2-yl]-benzamide 和 4-( tert -butyl)- N -{4-[(4-与 5-氟尿嘧啶相比，哌啶子哌啶-1-基)甲基]噻唑-2-基}苯甲酰胺具有相似的活性。含 4-piperidino-piperidin-1-yl 的衍生物还通过诱导细胞凋亡抑制培养的肿瘤细胞的增殖。