Journal
EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
Volume 114, Issue -, Pages 65-78Publisher
ELSEVIER FRANCE-EDITIONS SCIENTIFIQUES MEDICALES ELSEVIER
DOI: 10.1016/j.ejmech.2016.02.051
Keywords
AIDS; HIV-1; CXCR4; Small molecular; Entry inhibitors; Drug design
Categories
Funding
- Key Project of National Natural Science Foundation of China (NSFC) for International Cooperation [81420108027]
- National Natural Science Foundation of China [81273354]
- Research Fund for the Doctoral Program of Higher Education of China [20110131130005]
- Natural Science Foundation of Shandong Province [ZR2009CM016]
- Major Project of Science and Technology of Shandong Province [2015ZDJS04001]
- Science and Technology Development Project of Shandong Province [2012GSF11804]
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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.
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