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Indole-based allosteric inhibitors of HIV-1 integrase.
- Source :
-
Bioorganic & Medicinal Chemistry Letters . Oct2016, Vol. 26 Issue 19, p4748-4752. 5p. - Publication Year :
- 2016
-
Abstract
- 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 (IC 50 = 4.5 μM) 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. [ABSTRACT FROM AUTHOR]
Details
- Language :
- English
- ISSN :
- 0960894X
- Volume :
- 26
- Issue :
- 19
- Database :
- Academic Search Index
- Journal :
- Bioorganic & Medicinal Chemistry Letters
- Publication Type :
- Academic Journal
- Accession number :
- 117915640
- Full Text :
- https://doi.org/10.1016/j.bmcl.2016.08.037