title: New anthraquinone derivatives as inhibitors of the HIV-1 reverse transcriptase-associated ribonuclease H function.
abstract: 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.
authors.affiliation: Department of Life and Environmental Sciences, University of Cagliari, Monserrato, Italy. francescaesposito@hotmail.com
authors.forename: Francesca
authors.initials: F
authors.lastname: Esposito
authors.forename: Angela
authors.initials: A
authors.lastname: Corona
authors.forename: Luca
authors.initials: L
authors.lastname: Zinzula
authors.forename: Tatyana
authors.initials: T
authors.lastname: Kharlamova
authors.forename: Enzo
authors.initials: E
authors.lastname: Tramontano
mesh_terms: D000880:Anthraquinones / Q000737:chemistry* / Q000378:metabolism; D015497:HIV-1 / Q000201:enzymology*; D006801:Humans; D007700:Kinetics; D011485:Protein Binding; D011994:Recombinant Proteins / Q000037:antagonists & inhibitors / Q000096:biosynthesis / Q000235:genetics; D018894:Reverse Transcriptase Inhibitors / Q000737:chemistry* / Q000378:metabolism; D016914:Ribonuclease H / Q000037:antagonists & inhibitors* / Q000235:genetics / Q000378:metabolism
chemical_list: D000880:Anthraquinones; D011994:Recombinant Proteins; D018894:Reverse Transcriptase Inhibitors; D016914:Ribonuclease H