Design, synthesis, and evaluation of the anticancer properties of a novel series of carboxamides, sulfonamides, ureas, and thioureas derived from 1,2,4-oxadiazol-3-ylmethyl-piperazin-1-yl substituted with pyrazolo[1,5- a ]pyrimidine derivatives

Monatshefte Fur Chemie(2016)

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摘要
A series of novel carboxamides, sulfonamides, ureas, and thioureas derived from 1,2,4-oxadiazol-3-ylmethyl-piperazin-1-yl substituted with pyrazolo[1,5- a ]pyrimidine analog were designed and synthesized. The newly synthesized compounds were characterized by 1 H NMR, 13 C NMR, ESI–MS, and IR and were tested for their in vitro antiproliferative activity by MTT assay. Out of these twenty derivatives, five compounds showed good anticancer activity against HeLa cell line. These are superior with less than 10 µg/cm 3 of IC 50 when compared to the marketed anticancer drug paclitaxel with 30 µg/cm 3 of IC 50 against Hela cell line. Graphical abstract
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关键词
Carboxamide,Sulfonamide,Urea,Thiourea,Pyrazolo[1,5-a]pyrimidine,1,2,4-Oxadiazole,Piperazine,Anticancer activity
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