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dc.contributor.author
Won-Gil Lee  
dc.contributor.author
Frey, Kathleen M.  
dc.contributor.author
Ricardo Gallardo-Macias  
dc.contributor.author
Spasov, Krasimir A.  
dc.contributor.author
Bollini, Mariela  
dc.contributor.author
Anderson, Karen S.  
dc.contributor.author
Jorgensen, William L.  
dc.date.available
2019-10-16T20:43:00Z  
dc.date.issued
2014-11  
dc.identifier.citation
Won-Gil Lee; Frey, Kathleen M.; Ricardo Gallardo-Macias; Spasov, Krasimir A.; Bollini, Mariela; et al.; Picomolar inhibitors of HIV-1 reverse transcriptase: Design and crystallography of naphthyl phenyl ethers; American Chemical Society; ACS Medicinal Chemistry Letters; 5; 11; 11-2014; 1259-1262  
dc.identifier.issn
1948-5875  
dc.identifier.uri
http://hdl.handle.net/11336/86098  
dc.description.abstract
Catechol diethers that incorporate a 6-cyano-1-naphthyl substituent have been explored as non-nucleoside inhibitors of HIV-1 reverse transcriptase (NNRTIs). Promising compounds are reported that show midpicomolar activity against the wild-type virus and sub-20 nM activity against viral variants bearing Tyr181Cys and Lys103Asn mutations in HIV-RT. An X-ray crystal structure at 2.49 Å resolution is also reported for the key compound 6e with HIV-RT.  
dc.format
application/pdf  
dc.language.iso
eng  
dc.publisher
American Chemical Society  
dc.rights
info:eu-repo/semantics/openAccess  
dc.rights.uri
https://creativecommons.org/licenses/by-nc-sa/2.5/ar/  
dc.subject
ANTI-HIV AGENTS  
dc.subject
NNRTIS  
dc.subject
PROTEIN CRYSTALLOGRAPHY  
dc.subject.classification
Química Orgánica  
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Ciencias Químicas  
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CIENCIAS NATURALES Y EXACTAS  
dc.title
Picomolar inhibitors of HIV-1 reverse transcriptase: Design and crystallography of naphthyl phenyl ethers  
dc.type
info:eu-repo/semantics/article  
dc.type
info:ar-repo/semantics/artículo  
dc.type
info:eu-repo/semantics/publishedVersion  
dc.date.updated
2019-09-27T21:02:12Z  
dc.journal.volume
5  
dc.journal.number
11  
dc.journal.pagination
1259-1262  
dc.journal.pais
Estados Unidos  
dc.journal.ciudad
Washington DC  
dc.description.fil
Fil: Won-Gil Lee. University of Yale; Estados Unidos  
dc.description.fil
Fil: Frey, Kathleen M.. University of Yale; Estados Unidos  
dc.description.fil
Fil: Ricardo Gallardo-Macias. University of Yale; Estados Unidos  
dc.description.fil
Fil: Spasov, Krasimir A.. University of Yale; Estados Unidos  
dc.description.fil
Fil: Bollini, Mariela. Consejo Nacional de Investigaciones Científicas y Técnicas. Oficina de Coordinación Administrativa Houssay; Argentina. University of Yale; Estados Unidos  
dc.description.fil
Fil: Anderson, Karen S.. University of Yale; Estados Unidos  
dc.description.fil
Fil: Jorgensen, William L.. University of Yale; Estados Unidos  
dc.journal.title
ACS Medicinal Chemistry Letters  
dc.relation.alternativeid
info:eu-repo/semantics/altIdentifier/doi/http://dx.doi.org/10.1021/ml5003713  
dc.relation.alternativeid
info:eu-repo/semantics/altIdentifier/url/https://pubs.acs.org/doi/10.1021/ml5003713  

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