-transparent.png){kind=logo}
New indolylarylsulfones as highly potent and broad spectrum HIV-1 non-nucleoside reverse transcriptase inhibitors. 2014
Valeria Famiglini, and
Giuseppe La Regina, and
Antonio Coluccia, and
Sveva Pelliccia, and
Andrea Brancale, and
Giovanni Maga, and
Emmanuele Crespan, and
Roger Badia, and
Bonaventura Clotet, and
José A Esté, and
Roberto Cirilli, and
Ettore Novellino, and
Romano Silvestri
Istituto Pasteur - Fondazione Cenci Bolognetti, Dipartimento di Chimica e Tecnologie del Farmaco, Sapienza Università di Roma, Piazzale Aldo Moro 5, I-00185 Roma, Italy.
New indolylarylsulfone HIV-1 NNRTIs were synthesized to evaluate unexplored substitutions of the benzyl/phenylethyl group linked at the indole-2-carboxamide. Against the NL4-3 HIV-1 WT strain, 17 out 20 compounds were superior to NVP and EFV. Several compounds inhibited the K103N HIV-1 mutant strain at nanomolar concentration and were superior to EFV. Some derivatives were superior to EFV against the Y181C and L100I HIV-1 mutant strains. Against the NL4-3 HIV-1 strain, the enantiomers 24 and 25 showed small differences of activity. In contrast, 24 turned out significantly more potent than 25 against the whole panel of mutant HIV-1 strains. The docking studies suggested that the difference in the observed inhibitory activities of 24 and 25 against the K03N mutation could be due to a kinetic rather than affinity differences.
Related Publications
Valeria Famiglini, and
Giuseppe La Regina, and
Antonio Coluccia, and
Sveva Pelliccia, and
Andrea Brancale, and
Giovanni Maga, and
Emmanuele Crespan, and
Roger Badia, and
Bonaventura Clotet, and
José A Esté, and
Roberto Cirilli, and
Ettore Novellino, and
Romano Silvestri
January 2022,
Bioorganic & medicinal chemistry,
Valeria Famiglini, and
Giuseppe La Regina, and
Antonio Coluccia, and
Sveva Pelliccia, and
Andrea Brancale, and
Giovanni Maga, and
Emmanuele Crespan, and
Roger Badia, and
Bonaventura Clotet, and
José A Esté, and
Roberto Cirilli, and
Ettore Novellino, and
Romano Silvestri
March 2011,
Journal of medicinal chemistry,
Valeria Famiglini, and
Giuseppe La Regina, and
Antonio Coluccia, and
Sveva Pelliccia, and
Andrea Brancale, and
Giovanni Maga, and
Emmanuele Crespan, and
Roger Badia, and
Bonaventura Clotet, and
José A Esté, and
Roberto Cirilli, and
Ettore Novellino, and
Romano Silvestri
January 2018,
Antiviral chemistry & chemotherapy,
Valeria Famiglini, and
Giuseppe La Regina, and
Antonio Coluccia, and
Sveva Pelliccia, and
Andrea Brancale, and
Giovanni Maga, and
Emmanuele Crespan, and
Roger Badia, and
Bonaventura Clotet, and
José A Esté, and
Roberto Cirilli, and
Ettore Novellino, and
Romano Silvestri
February 2019,
ACS medicinal chemistry letters,
Valeria Famiglini, and
Giuseppe La Regina, and
Antonio Coluccia, and
Sveva Pelliccia, and
Andrea Brancale, and
Giovanni Maga, and
Emmanuele Crespan, and
Roger Badia, and
Bonaventura Clotet, and
José A Esté, and
Roberto Cirilli, and
Ettore Novellino, and
Romano Silvestri
September 2006,
Bioorganic & medicinal chemistry letters,
Valeria Famiglini, and
Giuseppe La Regina, and
Antonio Coluccia, and
Sveva Pelliccia, and
Andrea Brancale, and
Giovanni Maga, and
Emmanuele Crespan, and
Roger Badia, and
Bonaventura Clotet, and
José A Esté, and
Roberto Cirilli, and
Ettore Novellino, and
Romano Silvestri
December 2012,
Journal of medicinal chemistry,
Valeria Famiglini, and
Giuseppe La Regina, and
Antonio Coluccia, and
Sveva Pelliccia, and
Andrea Brancale, and
Giovanni Maga, and
Emmanuele Crespan, and
Roger Badia, and
Bonaventura Clotet, and
José A Esté, and
Roberto Cirilli, and
Ettore Novellino, and
Romano Silvestri
January 2011,
Current medicinal chemistry,
Valeria Famiglini, and
Giuseppe La Regina, and
Antonio Coluccia, and
Sveva Pelliccia, and
Andrea Brancale, and
Giovanni Maga, and
Emmanuele Crespan, and
Roger Badia, and
Bonaventura Clotet, and
José A Esté, and
Roberto Cirilli, and
Ettore Novellino, and
Romano Silvestri
July 2013,
ChemMedChem,
Valeria Famiglini, and
Giuseppe La Regina, and
Antonio Coluccia, and
Sveva Pelliccia, and
Andrea Brancale, and
Giovanni Maga, and
Emmanuele Crespan, and
Roger Badia, and
Bonaventura Clotet, and
José A Esté, and
Roberto Cirilli, and
Ettore Novellino, and
Romano Silvestri
December 2003,
Bioorganic & medicinal chemistry letters,
Valeria Famiglini, and
Giuseppe La Regina, and
Antonio Coluccia, and
Sveva Pelliccia, and
Andrea Brancale, and
Giovanni Maga, and
Emmanuele Crespan, and
Roger Badia, and
Bonaventura Clotet, and
José A Esté, and
Roberto Cirilli, and
Ettore Novellino, and
Romano Silvestri
August 2011,
Bioorganic & medicinal chemistry,
