title: Prevention of HIV-1 infection by platinum triazines.
abstract: To identify and explore the activity of compounds which may act as anti-HIV virucidal agents, we have investigated platinum compounds, especially those containing N-donor aromatic ligands. After screening over 70 related agents, including N-donor aromatic ligands and metal precursors, we have identified a novel class of platinum(II) complexes with 2-pyridyl-1,2,4-triazine derivatives and Pt(II) formulations with these derivatives (ptt compounds) as having the highest anti-HIV activity. The maximum activity was observed when the agents were added immediately post-infection. The ptt agents did not block cell fusion activity of HIV-1 Env proteins in cells bearing CD4X4 or CD4R5 receptors, indicating a lack of interaction with the Env protein. The ptt compounds exhibit low toxicity for human epithelial cells, and are thus promising candidates for use as microbicides or antiviral agents against HIV.
authors.affiliation: Department of Microbiology and Immunology and Emory Vaccine Center, Emory University, 1510 Clifton Road, Room 3001, Atlanta, GA 30322, USA.
authors.forename: A N
authors.initials: AN
authors.lastname: Vzorov
authors.forename: D
authors.initials: D
authors.lastname: Bhattacharyya
authors.forename: L G
authors.initials: LG
authors.lastname: Marzilli
authors.forename: R W
authors.initials: RW
authors.lastname: Compans
mesh_terms: D000818:Animals; D019380:Anti-HIV Agents / Q000737:chemistry / Q000494:pharmacology* / Q000633:toxicity; D002460:Cell Line; D004353:Drug Evaluation, Preclinical; D015658:HIV Infections / Q000517:prevention & control*; D054303:HIV Reverse Transcriptase / Q000037:antagonists & inhibitors; D015497:HIV-1; D007700:Kinetics; D008561:Membrane Fusion / Q000187:drug effects; D051379:Mice; D017671:Platinum Compounds / Q000737:chemistry / Q000494:pharmacology* / Q000633:toxicity; D014227:Triazines / Q000737:chemistry / Q000494:pharmacology* / Q000633:toxicity
chemical_list: D019380:Anti-HIV Agents; D017671:Platinum Compounds; D014227:Triazines; D054303:HIV Reverse Transcriptase