Design And Synthesis Of 1,2,3-Triazolo-corannulene Hybrids As Cytotoxic Agents

Cancer has been a group of diseases that creates serious threat to humanity health.Cancer has become a worldwide disease harming humanity health and life safety.Therefore,synthesizing high efficient,broad-spectrum and low toxic anticarcinogen and studying their anticancer activity is becoming a strategic task of new drug development.According to this,in this work,attention is paid to corannulene.Corannulene is the smallest curved polycyclic aromatic hydrocarbon which consists of five benzene rings installed on a five-membered ring in the core.Due to the curvature in its structure endowing the bowl-shaped compound unique electronic properties,it has drawn more and more attention.However,the poor solubility in aqueous solution limit the application of corannulene in the biological system.In order to overcome this short coming,based on the molecular structure of corannulene,a new kind of 1,2,3-triazolo-corannulene hybrids has been designed and synthesized by conjugating corannulene with sugar.These compounds were evaluated for their in vitro cytotoxic potential against various human cancer cell lines viz.liver?HepG2?cells.Through cytotoxicity test,we found our compounds exhibit anticancer activity.From previous work it is known that the compounds with aromatic ring,which have anticancer activity,can bind to DNA.The small molecule compounds may interact with DNA directly or indirectly in vivo,which may change DNA structure and induce oxidative damage to DNA,and then affect its function or genetic characteristic.Based on this consideration,to study the mode and mechanism of interaction between our compounds with DNA is of realistic significance.It may be usefully researching the impact of our compounds on the structure and function of DNA,mechanism of toxicity and eliminating the adverse reactions.In this work,1,2,3-triazolo-corannulene hybrids are designed and synthesized.All target compounds have been characterized by ¹H NMR,¹³C NMR and MS.