2. Academic Validation
  3. Indolyl aryl sulfones as HIV-1 non-nucleoside reverse transcriptase inhibitors: role of two halogen atoms at the indole ring in developing new analogues with improved antiviral activity

Indolyl aryl sulfones as HIV-1 non-nucleoside reverse transcriptase inhibitors: role of two halogen atoms at the indole ring in developing new analogues with improved antiviral activity

  • J Med Chem. 2007 Oct 4;50(20):5034-8. doi: 10.1021/jm070488f.
Giuseppe La Regina 1,  Antonio Coluccia,  Francesco Piscitelli,  Alberto Bergamini,  Anna Sinistro,  Antonella Cavazza,  Giovanni Maga,  Alberta Samuele,  Samantha Zanoli,  Ettore Novellino,  Marino Artico,  Romano Silvestri
Affiliations

Affiliation

  • 1 Istituto Pasteur--Fondazione Cenci Bolognetti, Dipartimento di Studi Farmaceutici, Sapienza Università di Roma, Piazzale Aldo Moro 5, I-00185 Roma, Italy.
PMID: 17803291 DOI: 10.1021/jm070488f
Abstract

Indolyl aryl sulfones bearing the 4,5-difluoro (10) or 5-chloro-4-fluoro (16) substitution pattern at the indole ring were potent inhibitors of HIV-1 WT and the NNRTI-resistant strains Y181C and K103N-Y181C. These compounds were highly effective against the 112 and the AB1 strains in lymphocytes and inhibited at nanomolar concentration the multiplication of the IIIBBa-L strain in macrophages. Compound 16 was exceptionally potent against RT WT and RTs carrying the K103N, Y181I, and L100I mutations.

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