Synthesis And Activity Studies Of Diphenyl-substituted Aminomethyl Triazole Derivatives

1,2,3-triazole compounds are an important class of heterocycles which have highly activity biologically and a wide range of applications.This class of compoumd show high anti-tumor,anti-viral,anti-fungal,anti-HIV,activity and effective in treating arthritis and neurological disorder.As recently been reported,combretastatin A4(CA4)derivatives which were modified by 1,2,3-triazole ring possessed significant anti-tumor activity.The studies on synthesis and bioassay of compounds are important for finding biologically potent novel functional entities.In this paper,45 novel diphenyl-substituted aminomethyl triazole derivatives were synthesized and the antitumor activitie of these compounds were also evaluated.The results and details are shown below:1.In this dissertation,a series of novel 1,2,3-triazol-tethered combretastatin analogues C were designed and synthesized via "Click Chemistry",sodium azide,3-bromo-propyne,propiolate,brominated aromatic benzene and aniline aryl compounds.Then,the compounds C were derived to compounds C' and C".The structures of compounds were determined by NMR and MS.2.The preliminary bioassay test indicated that some of them exihibited a certain antitumor activity in vitro by MTT assay.The best biological activity of compound was carried out to discuss interactions between molecule and protein via molecular docking.