Literature DB >> 15026063

6-aryl-2,4-dioxo-5-hexenoic acids, novel integrase inhibitors active against HIV-1 multiplication in cell-based assays.

Roberta Costi1, Roberto Di Santo, Marino Artico, Alessandra Roux, Rino Ragno, Silvio Massa, Enzo Tramontano, Massimiliano La Colla, Roberta Loddo, M Elena Marongiu, Alessandra Pani, Paolo La Colla.   

Abstract

A series of 6-aryl-2,4-dioxo-5-hexenoic acids, were synthesized and tested against HIV-1 in cell-based assays and against recombinant HIV-1 integrase (rIN) in enzyme assays. Compound 8a showed potent antiretroviral activity (EC(50)=1.5 microM) and significant inhibition against rIN (strand transfer: IC(50)=7.9 microM; 3'-processing: IC(50)=7.0 microM). A preliminary molecular modeling study was carried out to compare the spatial conformation of 8a with those of L-731988 (4) and 5CITEP (7) in the IN core.

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Year:  2004        PMID： 15026063     DOI： 10.1016/j.bmcl.2004.01.037

Source DB:  PubMed          Journal:  Bioorg Med Chem Lett        ISSN： 0960-894X            Impact factor:   2.823


  8 in total

1.  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.

Authors:  Roberta Costi; Mathieu Métifiot; Francesca Esposito; Giuliana Cuzzucoli Crucitti; Luca Pescatori; Antonella Messore; Luigi Scipione; Silvano Tortorella; Luca Zinzula; Ettore Novellino; Yves Pommier; Enzo Tramontano; Christophe Marchand; Roberto Di Santo
Journal:  J Med Chem       Date:  2013-11-05       Impact factor: 7.446

2.  Novel bifunctional quinolonyl diketo acid derivatives as HIV-1 integrase inhibitors: design, synthesis, biological activities, and mechanism of action.

Authors:  Roberto Di Santo; Roberta Costi; Alessandra Roux; Marino Artico; Antonio Lavecchia; Luciana Marinelli; Ettore Novellino; Lucia Palmisano; Mauro Andreotti; Roberta Amici; Clementina Maria Galluzzo; Lucia Nencioni; Anna Teresa Palamara; Yves Pommier; Christophe Marchand
Journal:  J Med Chem       Date:  2006-03-23       Impact factor: 7.446

Review 3.  Active site and allosteric inhibitors of the ribonuclease H activity of HIV reverse transcriptase.

Authors:  Angela Corona; Takashi Masaoka; Graziella Tocco; Enzo Tramontano; Stuart F J Le Grice
Journal:  Future Med Chem       Date:  2013-12       Impact factor: 3.808

4.  Quinolinonyl Non-Diketo Acid Derivatives as Inhibitors of HIV-1 Ribonuclease H and Polymerase Functions of Reverse Transcriptase.

Authors:  Antonella Messore; Angela Corona; Valentina Noemi Madia; Francesco Saccoliti; Valeria Tudino; Alessandro De Leo; Davide Ialongo; Luigi Scipione; Daniela De Vita; Giorgio Amendola; Ettore Novellino; Sandro Cosconati; Mathieu Métifiot; Marie-Line Andreola; Francesca Esposito; Nicole Grandi; Enzo Tramontano; Roberta Costi; Roberto Di Santo
Journal:  J Med Chem       Date:  2021-06-09       Impact factor: 7.446

5.  HIV-1 Reverse Transcriptase Still Remains a New Drug Target: Structure, Function, Classical Inhibitors, and New Inhibitors with Innovative Mechanisms of Actions.

Authors:  Francesca Esposito; Angela Corona; Enzo Tramontano
Journal:  Mol Biol Int       Date:  2012-06-20

6.  Inhibiting the HIV integration process: past, present, and the future.

Authors:  Roberto Di Santo
Journal:  J Med Chem       Date:  2013-09-25       Impact factor: 7.446

Review 7.  Recent advances in the discovery of small-molecule inhibitors of HIV-1 integrase.

Authors:  Eungi Choi; Jayapal Reddy Mallareddy; Dai Lu; Srikanth Kolluru
Journal:  Future Sci OA       Date:  2018-09-06

Review 8.  Integrase Inhibitor Prodrugs: Approaches to Enhancing the Anti-HIV Activity of β-Diketo Acids.

Authors:  Vasu Nair; Maurice Okello
Journal:  Molecules       Date:  2015-07-13       Impact factor: 4.411
  8 in total

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