Related Experiment Video
Updated: Jul 7, 2026

Rapid Screening of HIV Reverse Transcriptase and Integrase Inhibitors
Published on: April 9, 2014
Chromone and chromanone derivatives as strand transfer inhibitors of HIV-1 integrase
Jang Hyun Park1, Seung Uk Lee, Sang Hoon Kim
1Division of Life Sciences, Korea Institute of Science & Technology, Seoul 130-650, Korea.
Abstract:
HIV-1 integrase catalyzes terminal cleavage at the 3' end of the proviral DNA, removing a pair of bases and causing strand transfer by joining the 3' end to 5'-phosphates in the target DNA. Several aryl 1,3-diketo acids that can inhibit the strand transfer reaction of HIV-1 IN have been identified. Here we synthesized a new series of compounds with a chromone or chromanone ring as conformationally constrained scaffolds of 1,3-diketo acids, and then tested their ability to inhibit HIV-1 IN-mediated strand transfer. All compounds moderately inhibited HIV-1 IN activity, indicating that the conformational restriction of one keto group into a chromone or chromanone ring decreases inhibition of the HIV-1 IN strand transfer.
Related Concept Videos
Antiviral Nucleoside Inhibitors
Inhibitors of Virion Maturation and Assembly
Inhibitors of Viral Protein Synthesis
Eukaryotic Transcription Inhibitors
Eukaryotic transcription inhibitors usually contain two distinct domains, a DNA...
Inhibitors of Bacterial DNA Synthesis
Retrovirus Life Cycles

