Synthesis And Antitumor Activity Of Aloe Emodin Derivatives

Cancer has become the leading cause of death,second only to cardiovascular disease.From 1949 to 2014,the US Food and Drug Administration（FDA）approved about 150cancer drugs.However,most of the anticancer drugs in clinical use are toxic and expen-sive to patients,and have acquired resistance.Therefore,it is necessary to develop new anticancer drugs with low toxicity,low cost and high efficiency.Aloe emodin belongs to anthraquinone compounds,which is a kind of bioactive component extracted from aloe,rhubarb and cassia.In this paper,aloe emodin was modi-fied by Bromination and aziding.The compound 2a-2q was obtained by N-alkylation of indole and substituted indole under alkaline conditions.Finally,the two compounds were combined to produce compounds with 1,2,3-triazole structure.17 aloe emodin derivatives were obtained by clicking chemical method,The structure of the structure was determined by ¹H NMR,¹³C-NMR and HRMS.The target compounds（5a-5q）were measured at 40%by MTT method and etoposide as positive control drugμThe antitumor activity of MCF-7cells,Hep G2 cells and AGS cells was studied in vitro at the concentration of mol/l.The results of activity test showed that some derivatives showed good antitumor activity.We further evaluated the antiproliferative effects of 5h,5I and 5m,which had good initial screening activity on 8 kinds of tumor cells,including MCF-7 cells,Hep G2 cells,AGS cells,SKOV3 cells,He La cells,A549 cells,MGC-803 cells and Ha Cat cells.Among them,Compound 5h showed obvious antiproliferative activity against human breast cancer cell MCF-7 and human ovarian cancer cell SKOV3,with IC₅₀ values of 1.73μmol/l and 3.09μmol/L,respectively,and its activity was better than that of etoposide.