Rapid Construction of Alkynylamide-substituted α,β-Diamino Acid Derivatives for Drug Discovery
作者单位：Shanghai Engineering Research Center of Molecular Therapeutics and New Drug DevelopmentEast China Normal University
会议名称：《第十届全国化学生物学学术会议》
会议日期：2017年
学科分类：1007[医学-药学(可授医学、理学学位)] 10[医学]
基 金：Project supported by the National Natural Science Foundation of China (No. 21332003 and No. 21672066) STCSM (No. 15ZR1411000)
关 键 词：Alkyne α,β-Diamino acid derivatives Multi-component method Drug discovery
摘 要：Alkyne moieties widely exist in natural products isolated from plants and marine organisms and pharmaceuticals as important pharmacophores. Developing straightforward and convenient approaches to rapid access to complex molecules containing alkynes is in increasing demand. Here, we reported a rapid approach to alkynylamide-substituted α,β-diamino acid derivatives from simple staring materials（Scheme 1） by using our previous developed multi-component method. [1] The desired products were obtained in high yields and with high diastereoselectivity. The resulting products showed a wide range of good bioactivity for cancer cells in the phenotypic screening（Table 1 and Figure 1） and are promising used as hits in drug discovery.