Design,Synthesis And Antitumor Activity Of Pyrazoline And Thiazolo Triazolone Derivatives

In recent years,people who suffer from cancer are becoming incresingly young,and the incidence of the disease is also increasing.On the one hand,it is related to the pressure of the modern society,the fast pace of life,and the bad habits of life,such as staying up late,drinking,smoking and so on,and the deterioration of work and living environment.At present,there is no drug that can cure cancer.The death toll of cancer patients in China alone is as high as 5000 per day.There are a series of side effects of chemotherapy,radiotherapyies and other traditional therapies,such as hair loss,decreasing immunity and so on,which seriously affect the treatment and life of cancer patients.Based on a large number of papers,it is found that pyrazoline is a kind of structure with many biological activities.Pyrazoline has also made many achievements in its anti-tumor research.Therefore,8 kinds of pyrazoline structure compounds have been designed and synthesized.The antitumor activity was enhanced by introducing halogen atoms and acyl chloride groups.The anti tumor activity was preliminarily detected by MTT.All compounds were confirmed by 1H-NMR,and some compounds were further identified by 13C-NMR and HRMS.The results showed that the eight kinds of pyrazoline showed a certain antitumor activity.The antiproliferative activity of all the compounds to all cells was greater than that of the positive control drug DDP namely cisplatin,and the antiproliferative activity of 3a-f to two kinds of HeLa and SGC-7901 cells was significantly stronger than that of the positive control drug taxol,and the toxicity of 3e(2-chloro-l-(5-(4-chlorophenyl)-4,5-dihydro-3-(4-nitrophenyl)-1H-pyrazol-1-yl)ethan one)to HepG2 cells was similar to that of taxol.Most triazolothiazolone derivatives exhibit different degrees of antiproliferative activity,of which compounds 5p((Z)-5-(3-methoxy-4-acetoxybenzyl)-2-(4-pyridyl)thiazole[3,2-b][1,2,4]triazol-6(5H)-one)and 5q((Z)-5-(4-methoxy-3-acetoxybenzy l)-2-(4-py ridy l)thiazole[3,2-b][1,2,4]triazol-6(5H)-one)in eight kinds of human cancer cell lines was good.Among them,compound 5q has the strongest antiproliferative activity against human gastric cancer cell line SGC-7901,and its IC50 value is 41.5±13.6 μM,stronger than that of control drug DDP.