Synthesis and biological evaluation of novel antiviral agents as protein–protein interaction inhibitors

References

• Global HIV/AIDS Response. Epidemic update and health sector progress towards universal access progress report; 2011
   Google Scholar
• Mehellou Y, De Clercq E. Twenty-six years of anti-HIV drug discovery: where do we stand and where do we go? J Med Chem 2010;53:521–38
   PubMed Web of Science ®Google Scholar
• Sechi M, Rizzi G, Bacchi A, et al. Design and synthesis of novel dihydroquinoline-3-carboxylic acids as HIV-1 integrase inhibitors. Bioorg Med Chem 2009;17:2925–35
   PubMed Web of Science ®Google Scholar
• Katlama C, Murphy R. Emerging role of integrase inhibitors in the management of treatment-experienced patients with HIV infection. Ther Clin Risk Manag 2009;5:331–40
   PubMedGoogle Scholar
• Neamati N, Marchand C, Pommier Y. HIV-1 integrase inhibitors: past, present, and future. Adv Pharmacol 2000;49:147–65
   PubMedGoogle Scholar
• d’Angelo J, Mouscadet JF, Desmaele D, et al. HIV-1 integrase: the next target for AIDS therapy? Pathol Biol (Paris) 2001;49:237–46
   PubMed Web of Science ®Google Scholar
• Neamati N. A small-molecule antagonist of virion assembly. Expert Opin Investig Drugs 2001;10:1767–70
   PubMed Web of Science ®Google Scholar
• Anthony NJ. HIV-1 integrase: a target for new AIDS chemotherapeutics. Curr Top Med Chem 2004;4:979–90
   PubMed Web of Science ®Google Scholar
• Pommier Y, Johnson AA, Marchand C. Integrase inhibitors to treat HIV/AIDS. Nat Rev Drug Discov 2005;4:236–48
   PubMed Web of Science ®Google Scholar
• Busschots K, Voet A, De Maeyer M, et al. Identification of the LEDGF/p75 binding site in HIV-1 integrase. J Mol Biol 2007;365:1480–92
   PubMed Web of Science ®Google Scholar
• Greene WC, Debyser Z, Ikeda Y, et al. Novel targets for HIV therapy. Antiviral Res 2008;80:251–65
   PubMedGoogle Scholar
• Cherepanov P, Sun ZY, Rahman S, et al. Solution structure of the HIV-1 integrase-binding domain in LEDGF/p75. Nat Struct Mol Biol 2005;12:526–32
   PubMed Web of Science ®Google Scholar
• Al-Mawsawi LQ, Neamati N. Allosteric inhibitor development targeting HIV-1 integrase. ChemMedChem 2011;6:228–41
   PubMedGoogle Scholar
• De Luca L, Barreca ML, Ferro S, et al. Pharmacophore-based discovery of small-molecule inhibitors of protein–protein interactions between HIV-1 integrase and cellular cofactor LEDGF/p75. ChemMedChem 2009;4:1311–6
   PubMed Web of Science ®Google Scholar
• De Luca L, Ferro S, Gitto R, et al. Small molecules targeting the interaction between HIV-1 integrase and LEDGF/p75 cofactor. Bioorg Med Chem 2010;18:7515–21
   PubMed Web of Science ®Google Scholar
• De Luca L, Ferro S, Morreale F, Chimirri A. Inhibition of the interaction between HIV-1 integrase and its cofactor LEDGF/p75: a promising approach in anti-retroviral therapy. Mini Rev Med Chem 2011;11:714–27
   PubMed Web of Science ®Google Scholar
• De Luca L, Ferro S, Morreale F, et al. Inhibitors of the interactions between HIV-1 IN and the cofactor LEDGF/p75. ChemMedChem 2011;6:1184–91
   PubMedGoogle Scholar
• De Luca L, Ferro S, Morreale F, et al. Fragment hopping approach directed at design of HIV IN-LEDGF/p75 interaction inhibitors. J Enzyme Inhib Med Chem 2012. [Epub ahead of print]. doi:10.3109/14756366.2012.703184
   Google Scholar
• De Luca L, Gitto R, Christ F, et al. 4-[1-(4-Fluorobenzyl)-4-hydroxy-1H-indol-3-yl]-2-hydroxy-4-oxobut-2-enoic acid as a prototype to develop dual inhibitors of HIV-1 integration process. Antiviral Res 2011;92:102–7
   PubMed Web of Science ®Google Scholar
• Jones G, Willett P, Glen RC, et al. Development and validation of a genetic algorithm for flexible docking. J Mol Biol 1997;267:727–48
   PubMed Web of Science ®Google Scholar
• De Luca L, Morreale F, Chimirri A. Insight into the fundamental interactions between LEDGF binding site inhibitors and integrase combining docking and molecular dynamics simulations. J Chem Inf Model 2012;52:3245--54
   Google Scholar
• Cherepanov P, Ambrosio AL, Rahman S, et al. Structural basis for the recognition between HIV-1 integrase and transcriptional coactivator p75. Proc Natl Acad Sci USA 2005;102:17308–13
   PubMed Web of Science ®Google Scholar
• Accelrys, Catalyst: http://www.accelrys.com
   Google Scholar
• Sechi M, Bacchi A, Carcelli M, et al. From ligand to complexes: inhibition of human immunodeficiency virus type 1 integrase by beta-diketo acid metal complexes. J Med Chem 2006;49:4248–60
   PubMed Web of Science ®Google Scholar
• De Luca L, Barreca ML, Ferro S, et al. A refined pharmacophore model for HIV-1 integrase inhibitors: optimization of potency in the 1H-benzylindole series. Bioorg Med Chem Lett 2008;18:2891–5
   PubMed Web of Science ®Google Scholar
• Ferro S, Grazia SD, De Luca L, et al. Microwave assisted organic synthesis (MAOS) of small molecules as potential HIV-1 integrase inhibitors. Molecules 2011;16:6858–70
   Google Scholar
• De Luca L, De Grazia S, Ferro S, et al. HIV-1 integrase strand-transfer inhibitors: design, synthesis and molecular modeling investigation. Eur J Med Chem 2011;46:756–64
   PubMed Web of Science ®Google Scholar
• Ferro S, Barreca ML, De Luca L, et al. New 4-[(1-benzyl-1H-indol-3-yl)carbonyl]-3-hydroxyfuran-2(5H)-ones, beta-diketo acid analogs as HIV-1 integrase inhibitors. Arch Pharm (Weinheim) 2007;340:292–8
   PubMed Web of Science ®Google Scholar
• Al-Mawsawi LQ, Christ F, Dayam R, et al. Inhibitory profile of a LEDGF/p75 peptide against HIV-1 integrase: insight into integrase-DNA complex formation and catalysis. FEBS Lett 2008;582:1425–30
   PubMed Web of Science ®Google Scholar
• Ortuso F, Langer T, Alcaro S. GBPM: GRID-based pharmacophore model: concept and application studies to protein–protein recognition. Bioinformatics 2006;22:1449–55
   PubMed Web of Science ®Google Scholar
• Alcaro S, Artese A, Ceccherini-Silberstein F, et al. Computational analysis of Human Immunodeficiency Virus (HIV) Type-1 reverse transcriptase crystallographic models based on significant conserved residues found in Highly Active Antiretroviral Therapy (HAART)-treated patients. Curr Med Chem 2010;17:290–308
   PubMed Web of Science ®Google Scholar
• DeLano WL. The PyMOL Molecular Graphics System. San Carlos (CA): DeLano Scientific LLC; 2008. Available from: http://www.pymol.org
   Google Scholar