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Issue 10, 2016

Design, synthesis and biological evaluation of caffeoyl benzanilides as dual inhibitors of HIV integrase and CCR5

Author affiliations

Abstract

Novel series of caffeoyl benzanilide compounds as dual inhibitors of HIV-1 CCR5/IN were designed and synthesized. The biological results indicated that the acetylated compounds with double bonds were reduced, especially compound 9a, which showed potential activity against HIV-1 CCR5 tropic viruses with an EC50 value of 4.85 μM, as well as binding affinity with IN (KD 2.4 μM). Molecular modeling studies also suggested the possible binding mode of 9a with CCR5 and IN. These results indicated that 9a has the possibility of being a dual inhibitor of HIV-1.

Graphical abstract: Design, synthesis and biological evaluation of caffeoyl benzanilides as dual inhibitors of HIV integrase and CCR5

Supplementary files

Article information


Submitted
02 Jun 2016
Accepted
28 Jul 2016
First published
02 Aug 2016

Med. Chem. Commun., 2016,7, 2028-2032
Article type
Research Article

Design, synthesis and biological evaluation of caffeoyl benzanilides as dual inhibitors of HIV integrase and CCR5

X. Sun, N. Fan, W. Xu, Y. Sun, X. Xie, Y. Guo, L. Ma, J. Liu and X. Wang, Med. Chem. Commun., 2016, 7, 2028 DOI: 10.1039/C6MD00311G

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