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Synthesis And Anticancer Activity Of 1,3,4-Thiadiazole Derivatives Based On Quinazolinone

Posted on:2024-05-08Degree:MasterType:Thesis
Country:ChinaCandidate:Y L MenFull Text:PDF
GTID:2531307166474124Subject:Chemical engineering
Abstract/Summary:PDF Full Text Request
Cancer has been a major public health problem that poses a serious threat to human health.There are many drugs available clinically for cancer treatment,but most of the anti-cancer drugs have problems such as high side effects and poor selectivity.Therefore,it is particularly important to develop anti-cancer drugs with novel structures.It has been reported that quinazolinone derivatives have various biological activities,such as anticancer,antiviral,antibacterial and antifungal,et al.1,3,4-thiadiazole has a wide range of biological activities,such as anticancer,antifungal,antiviral,antidepressant and antiparasitic,et al.Anticancer activity has become the focus of research on quinazolinone and 1,3,4-thiadiazole derivatives.Based on the above bioactive characteristics,thirty-five novel 1,3,4-thiadiazole derivatives based on quinazolinone were designed and synthesized in this paper.Using5-fluorouracil(5-FU)as a positive control drug,the proliferation inhibitory activity in vitro against L929,A549,Hela and MCF-7 cells were tested using CCK-8 method.The test results showed that for Hela cells,compounds 5i,6a-6f,6h-6k,6m and6q revealed good anti-proliferative activity,and compound 6i dispalyed the strongest inhibitory effect with an IC50 value of 1.38μmol/L.For MCF-7 cells,most of the compounds exhibited milder antiproliferative effect.Compound 6s showed efficient anti-tumor activity with an IC50 value of 3.01μmol/L.For A549 cells,compared with5-FU(IC50=8.13μmol/L),compounds 5a,5c,5e,5f and 5i reflected better proliferation inhibition effect with IC50 values of 2.21,3.13,3.75,4.41 and 3.55μmol/L,respectively.All compounds exhibited lower cytotoxicity against normal cells L929compared to 5-FU.The above findings laid a good foundation for studying the structure-activity relationship and mechanism of action of these compounds.
Keywords/Search Tags:Quinazolinone, 1,3,4-Thiadiazole, Synthesis, Antitumor activity, Cytotoxicity
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