Title: Design, synthesis and biological evaluation of substituted guanidine indole derivatives as potential inhibitors of HIV-1 Tat-TAR interaction
Authors: Wang, Jun ×
Wang, Yan
Li, Zhenyu
Zhan, Peng
Bai, Rujun
Pannecouque, Christophe
Balzarini, Jan
De Clercq, Erik
Liu, Xinyong #
Issue Date: Oct-2014
Series Title: Medicinal chemistry (Shāriqah (United Arab Emirates)) vol:10 issue:7 pages:738-46
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 was designed, synthesized and evaluated for their in vitro HIV-1 and HIV-2 inhibitory activity using the IIIB strain and ROD strain, respectively. Preliminary biological evaluation indicated that three compounds exhibited marked inhibitory activity against 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.
ISSN: 1573-4064
Publication status: published
KU Leuven publication type: IT
Appears in Collections:Laboratory of Virology and Chemotherapy (Rega Institute)
Production Engineering, Machine Design and Automation (PMA) Section
× corresponding author
# (joint) last author

Files in This Item:
File Description Status SizeFormat
2014179.pdf Published 2353KbAdobe PDFView/Open Request a copy

These files are only available to some KU Leuven Association staff members


All items in Lirias are protected by copyright, with all rights reserved.

© Web of science