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.
Acknowledgements
The authors are very grateful to A Fravolini for his pioneering efforts in the quinolone field and to all the members of our group for productive discussions. We express sincere gratitude to our colleagues who devoted much effort to the biological characterization of the compounds here reviewed: the research groups of G Palù and M Palumbo (University of Padova, Italy) and the research group of E De Clercq and C Pannecouque, with special thanks to D Daelemans and M Stevens (Rega Institute for Medical Research, Katholieke Universiteit, Leuven, Belgium). We are also grateful to A Loregian (University of Padova, Italy) for studies on compound 22, and A Marcello (International Centre for Genetic Engineering and Biotechnology (ICGEB), Trieste, Italy) for studies on compound 19.
Financial & competing interests disclosure
Our research is supported by the MIUR (PRIN 1998–2006, Roma, Italy). The authors have no other relevant affiliation or financial involvement with any organization or entity with a financial interest in or financial conflict with the subject matter or materials discussed in the manuscript. This includes employment, consultancies, honoraria, stock ownership or options, expert testimony, grants or patents received or pending or royalties.
No written assistance was utilized in the production of this manuscript.
Notes
Data from Citation[99–102].