Studies On Synthesis And Antitumor Activity Of Aza-brazilin—1,2,3-Triazole Compounds

In the past two decades,the incidence of cancer in China has been increasing year by year.With the acceleration of aging process,the incidence and mortality rate of cancer in China will continue to rise,which will cause great harm to individuals,society and even the whole country.Therefore,it is urgent to find new and more effective anticancer drugs.Researchs have shown that Brazilian compounds,as well as derivatives containing 1,2,3-triazole structural units,have significant antitumor activity.Based on our recent studies,a series of aza-brazilin-1,2,3-triazole hybrids were synthesized by molecular hybridization,and their antitumor cytotoxic activity was studied in vitro.Studies will expect to led to the discovery of lead compounds with antitumor activity.This thesis is divided into two major chapters.The first chapter mainly reviewed the physiological activities of brazilian-type and aza-brazilin compounds,and compounds containing 1,2,3-triazole structural units in recent years.The second chapter studied the synthesis and antitumor activity of aza-brazilin—1,2,3-triazole hybrids.Thirty-two novel aza-brazilin—1,2,3-triazole compounds were synthesized by molecular hybridization,and the antitumor cytotoxic activity of the compounds was evaluated in vitro.Studies showed that with reference to the positive control DDP,compounds k3 and k10show better antitumor cytotoxic activity.Compound k3 displayed cytotoxic activity against liver cancer(SMMC-7721),lung cancer(A549),colon cancer(SW480),breast cancer(MCF-7).The IC50values of the four tumor cells were 7.53,11.46,16.35,and 10.82?.M,respectively.Compound k10 also inhibited SMMC-7721,A549,SW480,and MCF-7 tumor cells with IC50 values of 6.4,11.25,10.10,and 7.32,respectively.In summary,thirty-two novel aza-brazilin-1,2,3-triazole compounds were synthesized in this thesis,and the antitumor activity was evaluated in vitro.Two compounds showed good inhibitory activity against four kinds of tumor cells MCF-7,SMMC-7721,A549,SW480.On the basis of this thesis,these 32 compounds will be structurally modified or prepared as salts analyze their structure-activity relationship,in order to find the lead compounds for antitumor activity.