Synthesis and cytotoxicity study of N-benzyl-3, 5-bis(arylmethylene)-4-piperidones / 中国药学杂志

ABSTRACT

OBJECTIVE: To synthesize a kind of novel cytotoxin with multi-drug-resistance reverting properties and study their cytotoxicity. METHODS: The target compounds were obtained from N-benzyl-4-piperidones and benzaldehyde derivatives on the condition of 20°C, 7-8 h, taking dry hydrogen chloride as catalyst, using aldol condensation reaction, inspected by TLC and purified through recrystallization. RESULTS: Five N-benzyl-3, 5-bis(arylmethylene)-4-piperidone derivatives were synthesized. The yield was over 49%. Their structures were characterized by 1H-NMR, ESI-MS with melting points. The data of cytotoxicity was obtained. CONCLUSION: The synthetic route is convenient and efficient; The compounds had good inhibiting activity for a few kinds of tumor cells. Copyright 2012 by the Chinese Pharmaceutical Association.