About: Acyclic nucleoside thiophosphonates as potent inhibitors of HIV and HBV replication

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An Entity of Type : schema:ScholarlyArticle, within Data Space : wasabi.inria.fr associated with source document(s)

Attributes	Values
type	Academic Article research paper schema:ScholarlyArticle
isDefinedBy	Covid-on-the-Web dataset
title	Acyclic nucleoside thiophosphonates as potent inhibitors of HIV and HBV replication
Creator	Balzarini, Jan Canard, Bruno Neyts, Johan Alvarez, Karine Barral, Karine Durafour, Céline Payrot, Nadine Priet, Stéphane Roux, Loic Weck, Clément Zoulim, Fabien
source	Elsevier; Medline; PMC
abstract	9-[2-(Thiophosphonomethoxy)ethyl]adenine 3 and (R)-9-[2-(Thiophosphonomethoxy)propyl]adenine 4 were synthesized as the first thiophosphonate nucleosides bearing a sulfur atom at the α-position of the acyclic nucleoside phosphonates PMEA and PMPA. Thiophosphonates S-PMEA 3 and S-PMPA 4 were evaluated for in vitro activity against HIV-1 (subtypes A to G), HIV-2 and HBV-infected cells, and found to exhibit potent antiretroviral activity. We showed that their diphosphate forms S-PMEApp 5 and S-PMPApp 6 are readily incorporated by wild-type (WT) HIV-1 RT into DNA and act as DNA chain terminators. Compounds 3 and 4 were evaluated for in vitro activity against a broad panel of DNA and RNA viruses and displayed beside HIV a moderate activity against herpes simplex virus and vaccinia viruses. In order to measure enzymatic stabilities of the target derivatives 3 and 4, kinetic data and decomposition pathways were studied at 37 °C in several media.
has issue date	2011-07-01(xsd:dateTime)
bibo:doi	10.1016/j.ejmech.2011.06.034
bibo:pmid	21803462
has license	no-cc
schema:url	https://doi.org/10.1016/j.ejmech.2011.06.034
resource representing a document's title	Acyclic nucleoside thiophosphonates as potent inhibitors of HIV and HBV replication
has PubMed Central identifier	PMC7115536
has PubMed identifier	21803462
schema:publication	Eur J Med Chem
resource representing a document's body	covid:PMC7115536#body_text
is schema:about of	named entity 'potent' named entity 'replication' named entity 'HIV' named entity 'EC50' named entity '1H NMR' named entity '1H NMR' named entity 'l-glutamine' named entity 'syncitial' named entity 'Sindbis virus' named entity 'bicarbonate' named entity 'HBV' named entity 'Influenza' named entity 'HPLC' named entity 'white powder' named entity 'PMPA' named entity '31P NMR' named entity 'Vesicular Stomatitis' named entity 'adefovir dipivoxil' named entity 'HIV-1' named entity 'NtRTI' named entity 'Tenofovir' named entity 'EC50' named entity 'diphosphate' named entity 'EC50' named entity 'nucleotide analogs' named entity 'clades' named entity 'carbonyldiimidazole' named entity 'antiretroviral drugs' named entity 'PMPA' named entity '5.0' named entity 'CHbN' named entity 'NRTIs' named entity 'phosphorylated' named entity 'PMPA' named entity 'lithium aluminum hydride' named entity 'adenine' named entity 'HIV-2' named entity 'transfection' named entity 'antiviral activity' named entity 'anti-HIV' named entity '1.1' named entity 'PHA' named entity 'H-8' named entity '50/50' named entity 'HIV-1' named entity 'α-position' named entity 'PMPA' named entity 'IC50' named entity 'antiviral' named entity 'multiplicity of infection' named entity 'HBV' named entity 'virus' named entity 'PBMCs' named entity 'Human Immunodeficiency Virus' named entity 'virus' named entity 'heterocyclic' named entity 'cell morphology' named entity 'nephrotoxic' named entity 'viral DNA' named entity 'D2O' named entity 'Coxsackie virus' named entity 'HIV' named entity 'Vesicular stomatitis virus' named entity 'PMPA' named entity 'HBV' named entity 'nucleoside' named entity 'Coxsackie virus' named entity 'white powder' named entity 'cell cultures' named entity 'infection' named entity 'D2O' named entity 'quasispecies'

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