Synthesis And Biological Activity Of Pyrrole-indolin-2-one Derivatives

In recent years,the research of indole heterocyclic compounds has drawn great attention because of its broad spectrum of biological activities in anti-inflammatory,anti-bacterial and anti-tumor.Cancer,with a high mortality rate is a serious threat to human life and health,and the listed indoles drugs with its toxic side effects and anti-selectivity and other characteristics of the tumor has achieved remarkable results,including: Sunitinib,SU5416,SU6668,Vinblastine,Vincristine,Vinorelbine and the like.Therefore,the research on the design,synthesis and biological activity of indole compounds has become one of the hot topics in the field of medicine.In this dissertation,the progress and current situation of indole compounds in the field of pharmaceutical research and development are systematically discussed in this paper.A comprehensive literature review of the studies on derivatives of indole derivatives has been made.On this basis,we further find indole compounds with certain anti-tumor activity.Using indolone as the lead compound,the C-3 position of indolinone was introduced into pyrrole using "connection of substructure" and "bioisosterism",and the biologically active thiadiazole Azole,amide and other structural fragments,a total of 16 novel indole heterocyclic compounds were synthesized.In this paper,1HNMR,13 CNMR and MS were used to characterize the target compounds.And the antiproliferative activity in different human cancer cell lines was studied by changing various substitutions of the fluorenone and benzene ring systems.As PC-1 cells,Hela cells,Hep G2 cells,and A549 cells were selected.Preliminary analysis showed that when the concentration was 10 ug/m L,the inhibitory rates of the target compounds III-13 and III-15 against the four tumor cells reached more than80%,which was comparable to the positive control drug Sunitinib.