标题：Discovery of non-peptide small molecular CXCR4 antagonists as anti-HIV agents: Recent advances and future opportunities
作者：Zhang, Heng; Kang, Dongwei; Huang, Boshi; Liu, Na; Zhao, Fabao; Zhan, Peng; Liu, Xinyong
作者机构：[Zhang, Heng; Kang, Dongwei; Huang, Boshi; Liu, Na; Zhao, Fabao; Zhan, Peng; Liu, Xinyong] Shandong Univ, Dept Med Chem, Key Lab Chem Biol, Sch Pharma 更多
通讯作者：Zhan, P;Liu, XY
通讯作者地址：[Zhan, P; Liu, XY]Shandong Univ, Dept Med Chem, Key Lab Chem Biol, Sch Pharmaceut Sci,Minist Educ, 44 West Culture Rd, Jinan 250012, Shandong, Peoples 更多
来源：EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
关键词：AIDS; HIV-1; CXCR4; Small molecular; Entry inhibitors; Drug design
摘要：CXCR4 plays vital roles in HIV-1 life cycle for it's essential in mediating the interaction of host and virus and completing the entry process in the lifecycle of HIV-1 infection. Compared with some traditional targets, CXCR4 provides a novel and less mutated drug target in the battle against AIDS. Its antagonists have no cross resistance with other antagonists. Great achievements have been made recent years and a number of small molecular CXCR4 antagonists with diversity scaffolds have been discovered. In this review, recent advances in the discovery of CXCR4 antagonists with special attentions on their evolution and structure-activity relationships of representative CXCR4 antagonists are described. Moreover, some classical medicinal chemistry strategies and novel methodologies are also introduced. (C) 2016 Elsevier Masson SAS. All rights reserved.