Synthesis And Anticancer Activity Of Amide Derivatives Containing1,3,4-Thiadiazole And Pyrazole

1,3,4-thiadiazole is a kind of very important heterocyclic compound, whichcontains the structure of "N-C-S". The synthesis and application of1,3,4-thiadiazoleand their derivatives have attracted more and more attentions since their wide rangeof biological and pharmaceutical activities such as anti-depression, anti-tumor,antibacterial, anti-cancer, insecticidal, plant growth regulating and so on. Meanwhile,as an other useful nitrogen-containing heterocyclic compound, pyrazole compoundshave widely used in the field of pharmaceuticals and agriculture as enzyme inhibitors,anticancers, antioxidant, insecticides and herbicides due to their excellent biologicalactivities.Based on the principle of bioactive superposition, we introduced the1,3,4-thiadiazole ring into pyrazole compounds. Consequently, twenty-six novelamide derivatives containing1,3,4-thiadiazole and pyrazole were designed andsynthesized. The synthesis route was shown in scheme1. All these target productshave not been reported in literature, and their structures were confirmed by IR、1HNMR、13C NMR、31P NMR、ESI-MS and HRMS.Besides, the inhibitory effect of target compounds were evaluated against EC109,HepG2and MGC803cells by a MTT method. The preliminary bioassay showed thatmost of the title compounds exhibit relatively weak inhibitory effect against HepG2and MGC803cells; and none inhibitory effect against EC109cells. In particular,compound A1exhibit higher activity against MGC803with the IC50value of0.042μmol/mL and superior to the positive control drug5-fluorouracil with the IC50valueof0.082μmol/mL. Scheme1Synthetic route of compounds (A1~A26)...