title: 6-desfluoroquinolones as HIV-1 Tat-mediated transcription inhibitors.
abstract: The current anti-HIV treatments fail to completely eradicate the virus in HIV-infected individuals, mainly as a result of a small pool of latently infected cells. This issue, together with the emergence of multidrug-resistant viruses, clearly highlights the need to find additional strategies. An overview of the Tat-mediated transcription inhibitors 6-desfluoroquinolones (6-DFQs), identified by our group, is given in this review along with a critical appraisal of their advantages and drawbacks. Attempts are also made to place them within the context of new potential anti-HIV therapeutics. Due to their innovative mechanism of action, the 6-DFQs could be interesting candidates for use in association with the currently used cocktail of drugs. Their potential as antivirals deserves further investigation.
authors.affiliation: Dipartimento di Chimica e Tecnologia del Farmaco, Università di Perugia, Via del Liceo 1, 06123 Perugia, Italy. oriana.tabarrini@unipg.it
authors.forename: Oriana
authors.initials: O
authors.lastname: Tabarrini
authors.forename: Serena
authors.initials: S
authors.lastname: Massari
authors.forename: Violetta
authors.initials: V
authors.lastname: Cecchetti
mesh_terms: D000818:Animals; D019380:Anti-HIV Agents / Q000737:chemistry / Q000494:pharmacology*; D024841:Fluoroquinolones / Q000737:chemistry / Q000494:pharmacology*; D015658:HIV Infections / Q000188:drug therapy*; D015497:HIV-1 / Q000187:drug effects* / Q000235:genetics; D006801:Humans; D014158:Transcription, Genetic / Q000187:drug effects*; D054322:tat Gene Products, Human Immunodeficiency Virus / Q000378:metabolism*
chemical_list: D019380:Anti-HIV Agents; D024841:Fluoroquinolones; D054322:tat Gene Products, Human Immunodeficiency Virus