Design And Synthesis Of 1,2,4 - Oxadiazole - Substituted Hydrazide Compounds Of Procaspase - 3 Activator

In this thesis, the mechanism of cell apoptosis and its relevant proteins were introduced briefly. The progress of cell apoptosis inducer as anticancer drugs were described in detail. A new series of 1,2,4-oxadiazole substituted hydrazide derivatives as Procaspase-3 activator were designed and synthesized in this thesis.We took PAC-1,the small molecular Procaspase-3 activator, as our lead compound. Based on its structure-activity relationship, the substituted hydrazide and the piperazine ring were retained. Making reference to the small molecular Procaspase activator 3-aryl-5-aryl-1,2,4-oxadiazoles, A series of substituted hydrazide derivatives were designed. A synthetic route was developed, and the target compounds were synthesized from 4-(chloromethyl)benzonitrile, followed by alkylation, addition, cyclizition, substitution, condensation. All the 16 new compounds have not been reported in literatures.The structures of the target compounds were confirmed by 1H-NMR and MS.