3-杂环取代吲哚衍生物的合成与抗肿瘤活性研究进展  

Research advances on synthesis and antitumor activity of 3-heterocyclic substituted indole derivatives

作　　者：王钦 汪从雨 龙雪莎 王贞超[1,2,3] 欧阳贵平 WANG Qin;WANG Cong-yu;LONG Xue-sha;WANG Zhen-chao;OUYANG Gui-ping(School of Pharmaceutical Science,Guizhou University,Guiyang 550025,China;State Key Laboratory Breeding Base of Green Pesticide and Agricultural Bioengineering/Key Laboratory of Ministry of Education,Guizhou University,Guiyang 550025,China;Guizhou Engineering Laboratory for Synthetic Drugs,Guiyang 550025,China)

机构地区：[1]贵州大学药学院,贵州贵阳550025 [2]贵州大学绿色农药与农业生物工程教育部重点实验室,贵州贵阳550025 [3]贵州省合成药物工程实验室,贵州贵阳550025

出　　处：《化学研究与应用》2022年第9期1955-1964,共10页Chemical Research and Application

基　　金：国家自然科学基金项目(21867004,22007022)资助;贵州省科技计划项目(黔科合平台人才[2018]5781号)资助。

摘　　要：杂环是大部分天然产物、合成及半合成分子的关键分子组成部分,具有重要的生物活性。其中,五元环及六元环体系是抗肿瘤药物的重要支架,在3-取代吲哚药物设计中占据重要地位,表现出较好的肿瘤抑制活性。本文围绕近年来含五元环、六元环的3-取代杂环吲哚衍生物的抗肿瘤活性及其构效关系进行综述,以期为含杂环的吲哚衍生物的合成研究提供一定参考。Heterocyclic rings are the key molecular fragments of most natural products,synthetic and semi-synthetic molecules,and have important biological activities.Among them,five-membered ring and six-membered ring systems are important scaffolds for antitumor drugs,and play a critical role in the design of 3-substituted indole drugs,showing good tumor inhibition activity.The antitumor activities and structure-activity relationship of 3-substituted heterocyclic indole derivatives containing 5-membered rings and 6-membered rings in recent years were reviewed in this paper,in order to provide some reference for the synthesis of heterocyclic indole derivatives.

关 键 词：杂环 吲哚 生物活性 抗肿瘤 构效关系 

分 类 号：O626[理学—有机化学]