Chromenone derivatives as a versatile scaffold with dual mode of inhibition of HIV-1 reverse transcriptase-associated Ribonuclease H function and integrase activity.

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ID: 86354
2019
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Abstract
A number of compounds targeting different processes of the Human Immunodeficiency Virus type 1 (HIV-1) life cycle have been developed in the continuing fight against AIDS. Coumarin-based molecules already proved to act as HIV-1 Protease (PR) or Integrase (IN) inhibitors and also to target HIV-1 reverse transcriptase (RT), blocking the DNA-dependent DNA-polymerase activity or the RNA-dependent DNA-polymerase activity working as common NNRTIs. In the present study, with the aim to exploit a coumarin-based scaffold to achieve the inhibition of multiple viral coded enzymatic functions, novel 4-hydroxy-2H, 5H-pyrano (3, 2-c) chromene-2, 5-dione derivatives were synthesized. The modeling studies calculated the theoretical binding affinity of the synthesized compounds on both HIV-1 IN and RT-associated Ribonuclease H (RNase H) active sites, which was confirmed by biological assays. Our results provide a basis for the identification of dual HIV-1 IN and RT RNase H inhibitors compounds.
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Authors Esposito, Francesca;Ambrosio, Francesca Alessandra;Maleddu, Rita;Costa, Giosuè;Rocca, Roberta;Maccioni, Elias;Catalano, Raffaella;Romeo, Isabella;Eleftheriou, Phaedra;Karia, Denish C;Tsirides, Petros;Godvani, Nilesh;Pandya, Hetal;Corona, Angela;Alcaro, Stefano;Artese, Anna;Geronikaki, Athina;Tramontano, Enzo;
Journal European journal of medicinal chemistry
Year 2019
DOI
S0223-5234(19)30751-2
URL
Keywords
hiv-1 coumarin derivatives rnase h dual inhibitors integrase ledgf/p75 cellular cofactor

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