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Pure Appl. Chem., 2003, Vol. 75, No. 2-3, pp. 195-206

HIV-1 integrase inhibitors that block HIV-1 replication in infected cells. Planning synthetic derivatives from natural products

Roberto Di Santo1, Roberta Costi1, Marino Artico1, E. Tramontano2, P. La Colla2 and A. Pani2

1 Istituto Pasteur—Fondazione Cenci Bolognetti, Dipartimento di Studi Farmaceutici (Dip. 63), Università di Roma “La Sapienza”, Piazzale A. Moro 5, I-00185 Roma, Italy
2 Dipartimento di Biologia Sperimentale, Sezione di Microbiologia, Università di Cagliari, Cittadella Universitaria, SS 554, I-09042 Monserrato, Cagliari, Italy

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  • Di Santo Roberto: Inhibiting the HIV Integration Process: Past, Present, and the Future. J. Med. Chem. 2014, 57, 539. <>
  • Costi Roberta, Métifiot Mathieu, Esposito Francesca, Cuzzucoli Crucitti Giuliana, Pescatori Luca, Messore Antonella, Scipione Luigi, Tortorella Silvano, Zinzula Luca, Novellino Ettore, Pommier Yves, Tramontano Enzo, Marchand Christophe, Di Santo Roberto: 6-(1-Benzyl-1H-pyrrol-2-yl)-2,4-dioxo-5-hexenoic Acids as Dual Inhibitors of Recombinant HIV-1 Integrase and Ribonuclease H, Synthesized by a Parallel Synthesis Approach. J. Med. Chem. 2013, 56, 8588. <>
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  • Sahu Kamlesh Kumar, Ravichandran Veerasamy, Mourya Vishnu Kant, Agrawal Ram Kishore: QSAR analysis of caffeoyl naphthalene sulfonamide derivatives as HIV-1 integrase inhibitors. Med Chem Res 2007, 15, 418. <>
  • Veljkovic Veljko, Mouscadet Jean-François, Veljkovic Nevena, Glisic Sanja, Debyser Zeger: Simple criterion for selection of flavonoid compounds with anti-HIV activity. Biorg Med Chem Lett 2007, 17, 1226. <>
  • Nuttall Jeremy, Romano Joseph, Douville Karen, Galbreath Caroline, Nel Annaléne, Heyward William, Mitchnick Mark, Walker Saul, Rosenberg Zeda: The Future of HIV Prevention: Prospects for an Effective Anti-HIV Microbicide. Infect Dis Clin N Amer 2007, 21, 219. <>
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  • Di Santo R., Costi R., Artico M., Ragno R., Greco G., Novellino E., Marchand C., Pommier Y., Abdel-Ghani Nour T., Youssef Ahmed F.A., Awady Mohamed A., El-Gindy Alaa, Emara Samy, Mesbah Mostafa K., Hadad Ghada M.: Design, synthesis and biological evaluation of heteroaryl diketohexenoic and diketobutanoic acids as HIV-1 integrase inhibitors endowed with antiretroviral activity. Il Farmaco 2005, 60, 409. <>