| Design, synthesis, and anti-HIV activity of 2',3'-didehydro-2',3'-dideoxyuridine (d4U), 2',3'-dideoxyuridine (ddU) phosphoramidate 'ProTide' derivatives. | |
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MedLine Citation:
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PMID: 17485204 Owner: NLM Status: MEDLINE |
Abstract/OtherAbstract:
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We report the synthesis of 2',3'-didehydro-2',3'-dideoxyuridine (d4U) and 2',3'-dideoxyuridine (ddU) phosphoramidate 'ProTide' derivatives and their evaluation against HIV-1 and HIV-2. In addition, we conducted molecular modeling studies on both d4U and ddU monophosphates to investigate their second phosphorylation process. The findings from the modeling studies provide compelling evidence for the lack of anti-HIV activity of d4U phosphoramidates, in contrast with the corresponding ddU phosphoramidates. |
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Authors:
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Youcef Mehellou; Christopher McGuigan; Andrea Brancale; Jan Balzarini |
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Publication Detail:
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Type: Journal Article Date: 2007-04-22 |
Journal Detail:
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Title: Bioorganic & medicinal chemistry letters Volume: 17 ISSN: 0960-894X ISO Abbreviation: Bioorg. Med. Chem. Lett. Publication Date: 2007 Jul |
Date Detail:
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Created Date: 2007-06-18 Completed Date: 2007-09-06 Revised Date: - |
Medline Journal Info:
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Nlm Unique ID: 9107377 Medline TA: Bioorg Med Chem Lett Country: England |
Other Details:
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Languages: eng Pagination: 3666-9 Citation Subset: IM |
Affiliation:
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Welsh School of Pharmacy, Cardiff University, King Edward VII Avenue, Cardiff, UK. |
Export Citation:
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| MeSH Terms | |
Descriptor/Qualifier:
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Amides
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chemistry* Anti-HIV Agents / chemical synthesis*, chemistry Chemistry, Pharmaceutical / methods* Dideoxynucleosides / chemical synthesis*, chemistry* Drug Design HIV-1 / metabolism HIV-2 / metabolism Models, Chemical Models, Molecular Nucleoside-Phosphate Kinase / chemistry Nucleosides / chemistry Phosphates / chemistry Phosphoric Acids / chemistry* Phosphorylation Thymidine Monophosphate / chemistry |
| Chemical | |
Reg. No./Substance:
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0/Amides; 0/Anti-HIV Agents; 0/Dideoxynucleosides; 0/Nucleosides; 0/Phosphates; 0/Phosphoric Acids; 2817-45-0/phosphoramidic acid; 365-07-1/Thymidine Monophosphate; 5974-93-6/2',3'-didehydro-2',3'-dideoxyuridine; 5983-09-5/2',3'-dideoxyuridine; EC 2.7.4.4/Nucleoside-Phosphate Kinase; EC 2.7.4.9/dTMP kinase |
From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine
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