Synthesis And Bioactivity Of 4-Aryl-5-(1H-1,2,4-triazol-1-yl)-2-aminothiazole Derivatives

Acetophenone,have a variety of biological and pharmacological activities.Therefore,acetophenone skeleton was chosen as an active pharmacal core to screen for new potential antitumor compounds by the introduction of various bioactive functional groups,such as 1H-1,2,4-triazole,arylaminothiazoles and thiazole schiff bases.In this paper,two series of anti cancer agents were designed and synthesized.The compounds 5 and 6 were synthesized from the key intermediate 2-bromo-2-(1H-1,2,4-triazol-1-yl)-1-phenylethanone(3).All of these target compounds were characterized by 1H NMR,and evaluated for anticancer activities against human cancer cell lines.Among them,the most potent compounds were further investigated their interactions with ctDNA by fluorescence spectrum.1.Synthesis and biological activity of(E)-4-aryl-2-(2-hydroxy-benzylidene-amino)-5-(1H-1,2,4-triazol-1-yl)thiazole(5)Based on our previous work,acetophenone was selected as pharmacal core to design and synthesize a series of new acetophenone derivatives bearing thiazoles schiff bases as antitumor agents.Therefore,a series of(E)-4-aryl-2-(2-hydroxybenzylideneamino)-5-(1H-1,2,4-triazol-1-yl)thiazole(5)were synthesized and evaluated their potential anti cancer activity against two human cancer cell lines.The most potent compound 51 demonstrated moderate activities against A549 and Hela cells with the inhibition rates of 51.76%and 52.02%at 10μM,respectively.2.Synthesis and anticancer activity of 4-aryl-5-(1,2,4-triazol-1-yl)-2-arylamino thiazole(6)Acetophenone was chosen as an active pharmacal core to screen for new potential antitumor compounds by the introduction of 1H-1,2,4-triazole and arylaminothiazoles.A series of 4-aryl-5-(1H-1,2,4-triazol-1-yl)-2-arylamino thiazole(6)were synthesized and evaluated for their potential anticancer activity against three human cancer cell lines in vitro.Among them,compound 6n showed the best results,with good inhibitory activity against A549,Hela and MCF-7 cells with the inhibition rates of 53.14%,67.08%and 76.86%at 10μM,respectively.