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Updated: May 17, 2026

Quantitative Structure-Activity Relationship, Activity Prediction, and Molecular Dynamics of Non-nucleotide Reverse Transcriptase Inhibitors
Published on: May 9, 2025
New anthraquinone derivatives as inhibitors of the HIV-1 reverse transcriptase-associated ribonuclease H function
Francesca Esposito1, Angela Corona, Luca Zinzula
1Department of Life and Environmental Sciences, University of Cagliari, Monserrato, Italy. francescaesposito@hotmail.com
Background:
The degradative activity of the human immunodeficiency virus type 1 (HIV-1) reverse transcriptase (RT), termed ribonuclease H (RNase H), which hydrolyzes the RNA component of the heteroduplex RNA:DNA replication intermediate, is an excellent target for drug discovery. Anthraquinones (AQs) and their derivatives, which are common secondary metabolites occurring in bacteria, fungi, lichens and a large number of families in higher plants, have been reported to have several biological activities including that of inhibiting HIV-1 RT activities in biochemical assays.
Methods:
We have assayed new AQ derivatives on HIV-1 RNase H activities in biochemical assays.
Results:
Six series of new AQ derivatives with various substituents at positions 1, 2, 3 and 4 of the AQ ring were tested, and new analogs able to inhibit HIV-1 RT-associated RNase H activity in the low micromolar range were found.
Conclusions:
Our results demonstrate that AQ derivatives are promising anti-RNase H inhibitors.
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