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Title: Indolylarylsulfones as HIV-1 non-nucleoside reverse transcriptase inhibitors: new cyclic substituents at indole-2-carboxamide
Authors: La Regina, Giuseppe ×
Coluccia, Antonio
Brancale, Andrea
Piscitelli, Francesco
Gatti, Valerio
Maga, Giovanni
Samuele, Alberta
Pannecouque, Christophe
Schols, Dominique
Balzarini, Jan
Novellino, Ettore
Silvestri, Romano #
Issue Date: Mar-2011
Publisher: ACS Publications
Series Title: Journal of Medicinal Chemistry vol:54 issue:6 pages:1587-1598
Abstract: New indolylarylsulfone derivatives bearing cyclic substituents at indole-2-carboxamide linked through a methylene/ethylene spacer were potent inhibitors of the WT HIV-1 replication in CEM and PBMC cells with inhibitory concentrations in the low nanomolar range. Against the mutant L100I and K103N RT HIV-1 strains in MT-4 cells, compounds 20, 24-26, 36, and 40 showed antiviral potency superior to that of NVP and EFV. Against these mutant strains, derivatives 20, 24-26, and 40 were equipotent to ETV. Molecular docking experiments on this novel series of IAS analogues have also suggested that the H-bond interaction between the nitrogen atom in the carboxamide chain of IAS and Glu138:B is important in the binding of these compounds. These results are in accordance with the experimental data obtained on the WT and on the mutant HIV-1 strains tested.
URI: 
ISSN: 0022-2623
Publication status: published
KU Leuven publication type: IT
Appears in Collections:Laboratory of Virology and Chemotherapy (Rega Institute)
× corresponding author
# (joint) last author

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