Indole-based allosteric inhibitors of HIV-1 integrase
Copyright policy )Indole-based allosteric inhibitors of HIV-1 integrase
Employing a scaffold hopping approach, a series of allosteric HIV-1 integrase (IN) inhibitors (ALLINIs) have been synthesized based on an indole scaffold. These compounds incorporate the key elements utilized in quinoline-based ALLINIs for binding to the IN dimer interface at the principal LEDGF/p75 binding pocket. The most potent of these compounds displayed good activity in the LEDGF/p75 dependent integration assay (IC50=4.5μM) and, as predicted based on the geometry of the five- versus six-membered ring, retained activity against the A128T IN mutant that confers resistance to many quinoline-based ALLINIs.
- The Ohio State University United States
- University of California, San Diego United States
- University of Southern Mississippi United States
- Helwan University Egypt
Scaffold hopping, Indoles, 610, Hydrogen Bonding, HIV Integrase, 540, Crystallography, X-Ray, Structure-Activity Relationship, Allosteric Regulation, ALLINI, HIV Integrase Inhibitors, HIV integrase inhibitor
Scaffold hopping, Indoles, 610, Hydrogen Bonding, HIV Integrase, 540, Crystallography, X-Ray, Structure-Activity Relationship, Allosteric Regulation, ALLINI, HIV Integrase Inhibitors, HIV integrase inhibitor
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