Design, Synthesis and Biological Evaluation of Substituted Guanidine Indole Derivatives as Potential Inhibitors of HIV-1 Tat–TAR Interaction

ISSN: 1875-6638 (Online)
ISSN: 1573-4064 (Print)


Volume 10, 8 Issues, 2014


Download PDF Flyer




Medicinal Chemistry

Aims & ScopeAbstracted/Indexed in


Submit Abstracts Online Submit Manuscripts Online

Editor-in-Chief:
Atta-ur-Rahman, FRS
Honorary Life Fellow
Kings College
University of Cambridge
Cambridge
UK
Email: mc@benthamscience.org

View Full Editorial Board

Subscribe Purchase Articles Order Reprints

Current: 1.387
5 - Year: 1.379

Design, Synthesis and Biological Evaluation of Substituted Guanidine Indole Derivatives as Potential Inhibitors of HIV-1 Tat–TAR Interaction

Author(s): Jun Wang, Yan Wang, Rujun Bai, Peng Zhan, Christophe Pannecouque, Jan Balzarini, Erik De Clercq and Xinyong Liu

Affiliation: Key Laboratory of Chemical Biology(Educational Ministry of China)and Department of medicinal Chemistry, School of Pharmaceutical Sciences, Shandong University, No.44 Wenhuaxi Road, Jinan 250012, China

Abstract

The interaction between the HIV-1 transactivator protein Tat and RNA response element (TAR) plays a critical role in HIV-1 transcription. Based on the pharmacophore model of reported inhibitors, a series of novel substituted guanidine indole derivatives were designed, synthesized and evaluated for their in vitro HIV-1 and HIV-2 activity using the IIIB strain and ROD strain, respectively. Preliminary biological evaluation indicated that three compounds exhibited marked inhibitory activity HIV-1 IIIB. Quite unexpectedly, compound a-7 was also endowed with the moderate anti-HIV-2 potency (EC50 = 58.14 μM). In addition, preliminary discussion on the activity results and molecular modeling of these new analogues were presented in this manuscript

Keywords: Drug Design, Guanidine Indole Synthesis, HIV-1 Tat, HIV-1 TAR, Inhibitors

Purchase Online Rights and Permissions

  
  



Article Details

Volume: 10
First Page: 1
Last Page: 9
Page Count: 9
DOI: 10.2174/1573406410666140306151815
Advertisement

Related Journals




Webmaster Contact: urooj@benthamscience.org Copyright © 2014 Bentham Science