Artículo
Picomolar inhibitors of HIV-1 reverse transcriptase: Design and crystallography of naphthyl phenyl ethers
Won-Gil Lee; Frey, Kathleen M.; Ricardo Gallardo-Macias; Spasov, Krasimir A.; Bollini, Mariela
; Anderson, Karen S.; Jorgensen, William L.
Fecha de publicación:
11/2014
Editorial:
American Chemical Society
Revista:
ACS Medicinal Chemistry Letters
ISSN:
1948-5875
Idioma:
Inglés
Tipo de recurso:
Artículo publicado
Clasificación temática:
Resumen
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.
Palabras clave:
ANTI-HIV AGENTS
,
NNRTIS
,
PROTEIN CRYSTALLOGRAPHY
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Identificadores
Colecciones
Articulos(OCA HOUSSAY)
Articulos de OFICINA DE COORDINACION ADMINISTRATIVA HOUSSAY
Articulos de OFICINA DE COORDINACION ADMINISTRATIVA HOUSSAY
Citación
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
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