Target-based anticancer indole derivatives and insight into structure-activity relationship:A mechanistic review update(2018—2021)

作     者：Ashima Dhiman Rupam Sharma Rajesh K.Singh Ashima Dhiman;Rupam Sharma;Rajesh K.Singh

作者机构：Department of Pharmaceutical ChemistryShivalik College of PharmacyIKG Punjab Technical UniversityJalandhar 140126India 

出 版 物：《Acta Pharmaceutica Sinica B》 (药学学报（英文版）)

年 卷 期：2022年第12卷第7期

页      面：3006-3027页

核心收录：

学科分类：1007[医学-药学(可授医学、理学学位)] 10[医学] 

基　　金：the Managing Committee of Shivalik College of Pharmacy 

主　　题：Indole Synthesis Anticancer Structure-activity relationship Topoisomerase Apoptosis Aromatase inhibitors Tubulin inhibitors 

摘      要：Cancer,which is the uncontrolled growth of cells,is the second leading cause of death after heart *** drugs,especially to specific genes and proteins involved in growth and survival of cancer cells,is the prime need of research *** moiety,which is a combination of aromatic-heterocyclic compounds,is a constructive scaffold for the development of novel *** to its bioavailability,high unique chemical properties and significant pharmacological behaviours,indole is considered as the most inquisitive scaffold for anticancer drug *** is illustrated by the fact that the *** and Drug Administration(FDA)has recently approved several indole-based anticancer agents such as panobinostat,alectinib,sunitinib,osimertinib,anlotinib and nintedanib for clinical ***,hundreds of studies on the synthesis and activity of the indole ring have been published in the last three *** into account the facts stated above,we have presented the most recent advances in medicinal chemistry of indole derivatives,encompassing hot articles published between 2018and 2021 in anticancer drug *** recent advances made towards the synthesis of promising indole-based anticancer compounds that may act via various targets such as topoisomerase,tubulin,apoptosis,aromatase,kinases,etc.,have been *** review also summarizes some of the recent efficient green chemical synthesis for indole rings using various catalysts for the period during 2018—*** review also covers the synthesis,structure-activity relationship,and mechanism by which these leads have demonstrated improved and promising anticancer *** molecules under clinical and preclinical stages are classified into groups based on their cancer targets and presented in tabular form,along with their mechanism of *** goal of this review article is to point the way for medicinal chemists to design and develop effective indole-based anticancer agents.