Synthesis And Anticancer Activity Of 1,3,4-Oxadiazole And 1,2,4-Triazole Derivatives Based On Quinazolinone

Cancer causes cells to divide and grow abnormally,then spread to other parts of the body,which can have a serious impact on health.New antitumor compounds have strong selective anticancer effects,and must exhibit a cytotoxic effect on malignant cells,without damaging normal cells.it was reported that the quinazolinone derivatives possess antitumor,antituberculosis,antioxidant,anti-inflammatory and antibacterial activities,et al.A number of 1,3,4-oxadiazole and 1,3,4-thiazole derivatives were reported to possess a wide range of biological activities such as antiviral,anti-inflammatory,antitumor and antioxidant effects,et al.Based on the above reports,a serious of new 1,3,4-oxadiazole and 1,2,4-triazole derivatives linked to quinazolinone were designed and synthesized,and CCK-8 assay was used to detect their in vitro antiproliferative activities against A549,Hela,L929and MCF-7.Compounds 9m,9b and 8o showed good antiproliferative activity against A549cells with IC₅₀ values of 2.96,3.46 and 3.44μmol/L respectively.Compounds 9h and9m had strong inhibitory effects on Hela cells,with IC₅₀ values of 1.76 and 3.91μmol/L.Compound 9i showed high inhibitory activity against MCF-7 cells with IC₅₀ value of2.72μmol/L.Meanwhile,all compounds showed lower cytotoxicity to L929 cells than5-fluorouracil.In summary,thirty 1,3,4-oxadiazole and 1,2,4-triazole derivatives linked to quinazolinone all showed different degrees of anticancer activity against A549,Hela and MCF-7 cells,and compared with 5-fluorouracil,all compounds exhibited lower cytotoxicity against L929 cells.