SYNTHESIS AND CYTOTOXIC ACTIVITY OF AZA-MICHAEL REACTION PRODUCTS FROM ETHYL SORBATE AND HETEROCYCLIC AMINES

摘要

The solvent-free reaction of ethyl sorbate and several heterocyclic amines at room temperature was shown to give aza-Michael 1,4-addition products. The newly formed double bond in the principal product had the E-configuration. It was found that the synthesized compounds exhibited cytotoxicity against cancer cell lines CEM-13, U-937, and MT-4. The piperazine derivative of ethyl sorbate exhibited the greatest activity against cancer cell line U-937, for which the concentration causing 50% death of the tumor cells (CTD50) was 10 mu g/mL.