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EnglishBackground: 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.
New anthraquinone derivatives as inhibitors of the HIV-1 reverse transcriptase-associated ribonuclease H function / Esposito, Francesca; Corona, Angela; Zinzula, Luca; Kharlamova, Tatyana; Tramontano, Enzo. - In: CHEMOTHERAPY. - ISSN 0009-3157. - 58:4(2012), pp. 299-307.
| Titolo: | New anthraquinone derivatives as inhibitors of the HIV-1 reverse transcriptase-associated ribonuclease H function |
| Autori: | |
| Data di pubblicazione: | 2012 |
| Rivista: | |
| Citazione: | New anthraquinone derivatives as inhibitors of the HIV-1 reverse transcriptase-associated ribonuclease H function / Esposito, Francesca; Corona, Angela; Zinzula, Luca; Kharlamova, Tatyana; Tramontano, Enzo. - In: CHEMOTHERAPY. - ISSN 0009-3157. - 58:4(2012), pp. 299-307. |
| Handle: | http://hdl.handle.net/11584/175761 |
| Tipologia: | 1.1 Articolo in rivista |
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