Title: New nitrogen containing substituents at the indole-2-carboxamide yield high potent and broad spectrum indolylarylsulfone HIV-1 non-nucleoside reverse transcriptase inhibitors
Authors: La Regina, Giuseppe ×
Coluccia, Antonio
Brancale, Andrea
Piscitelli, Francesco
Famiglini, Valeria
Cosconati, Sandro
Maga, Giovanni
Samuele, Alberta
Gonzalez, Emmanuel
Clotet, Bonaventura
Schols, Dominique
Esté, José A
Novellino, Ettore
Silvestri, Romano #
Issue Date: Jul-2012
Publisher: ACS Publications
Series Title: Journal of Medicinal Chemistry vol:55 issue:14 pages:6634-6638
Abstract: New indolylarylsulfone (IAS) derivatives bearing nitrogen containing substituents at the indole-2-carboxamide inhibited the HIV-1 WT in MT-4 cells at low nanomolar concentrations. In particular, compound 9 was uniformly effective against the mutant Y181C, Y188L, and K103N HIV-1 strains; it was highly active against the multidrug resistant mutant IRLL98 HIV-1 strain bearing the K101Q, Y181C, and G190A mutations conferring resistance to NVP, DLV, and EFV and several HIV-1 clades A in PBMC.
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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