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4-Substituted 2-Hydroxyisoquinoline-1,3(2H,4H)-diones as a Novel Class of HIV-1 Integrase Inhibitors.
| dc.rights.license | open | en_US |
| dc.contributor.author | BILLAMBOZ, Muriel | |
| dc.contributor.author | SUCHAUD, Virginie | |
| dc.contributor.author | BAILLY, Fabrice | |
| dc.contributor.author | LION, Cedric | |
| dc.contributor.author | DEMEULEMEESTER, Jonas | |
| dc.contributor.author | CALMELS, Christina | |
| hal.structure.identifier | Microbiologie Fondamentale et Pathogénicité [MFP] | |
| dc.contributor.author | ANDRÉOLA, Marie-Line | |
| dc.contributor.author | CHRIST, Frauke | |
| dc.contributor.author | DEBYSER, Zeger | |
| dc.contributor.author | COTELLE, Philippe | |
| dc.date.accessioned | 2024-03-11T15:45:28Z | |
| dc.date.available | 2024-03-11T15:45:28Z | |
| dc.date.issued | 2013-07-11 | |
| dc.identifier.issn | 1948-5875 | en_US |
| dc.identifier.uri | https://oskar-bordeaux.fr/handle/20.500.12278/188691 | |
| dc.description.abstractEn | A series of 2-hydroxy-1,3-dioxoisoquinoline-4-carboxamides featuring an N-hydroxyimide chelating functionality was evaluated for their inhibitory properties against human immunodeficiency virus type 1 integrase (HIV-1 IN). Several derivatives displayed low nanomolar IC50 values comparable to that of the clinically used raltegravir. A marked effect of one compound on both primary IN-catalyzed reactions, strand transfer (ST), and 3' processing (3'-P), emphasizes a novel IN inhibition mechanism establishing it as a potential new generation IN inhibitor. Substitution of the 2-hydroxyisoquinoline-1,3-dione scaffold at position 4 by carboxamido chains was beneficial for antiviral activity since reproducible low micromolar anti-HIV activities were obtained for the first time within this scaffold. | |
| dc.language.iso | EN | en_US |
| dc.subject.en | 2-hydroxy-1 | |
| dc.subject.en | 3-dioxoisoquinoline-4-carboxamide; 3′ processing; HIV; antiretroviral; integrase | |
| dc.title.en | 4-Substituted 2-Hydroxyisoquinoline-1,3(2H,4H)-diones as a Novel Class of HIV-1 Integrase Inhibitors. | |
| dc.title.alternative | ACS Med Chem Lett | en_US |
| dc.type | Article de revue | en_US |
| dc.identifier.doi | 10.1021/ml400009t | en_US |
| dc.subject.hal | Sciences du Vivant [q-bio]/Microbiologie et Parasitologie | en_US |
| dc.identifier.pubmed | 24900718 | en_US |
| bordeaux.journal | ACS Medicinal Chemistry Letters | en_US |
| bordeaux.page | 606-11 | en_US |
| bordeaux.volume | 4 | en_US |
| bordeaux.hal.laboratories | MFP (Laboratoire Microbiologie Fondamentale et Pathogénicité) - UMR 5234 | en_US |
| bordeaux.issue | 7 | en_US |
| bordeaux.institution | CNRS | en_US |
| bordeaux.peerReviewed | oui | en_US |
| bordeaux.inpress | non | en_US |
| bordeaux.import.source | pubmed | |
| hal.identifier | hal-04454591 | |
| hal.version | 1 | |
| hal.date.transferred | 2024-03-11T15:45:31Z | |
| hal.popular | non | en_US |
| hal.audience | Internationale | en_US |
| hal.export | true | |
| workflow.import.source | pubmed | |
| dc.rights.cc | Pas de Licence CC | en_US |
| bordeaux.COinS | ctx_ver=Z39.88-2004&rft_val_fmt=info:ofi/fmt:kev:mtx:journal&rft.jtitle=ACS%20Medicinal%20Chemistry%20Letters&rft.date=2013-07-11&rft.volume=4&rft.issue=7&rft.spage=606-11&rft.epage=606-11&rft.eissn=1948-5875&rft.issn=1948-5875&rft.au=BILLAMBOZ,%20Muriel&SUCHAUD,%20Virginie&BAILLY,%20Fabrice&LION,%20Cedric&DEMEULEMEESTER,%20Jonas&rft.genre=article |
