Synthetic studies on the preparation of alanyl epoxysulfones as cathepsin cysteine protease electrophilic traps
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Otros documentos de la autoría: Latorre, Antonio; Rodríguez, Santiago; González, Florenci; Florea, Bogdan I.; Overkleeft, Herman S.
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Mostrar el registro completo del ítemcomunitat-uji-handle:10234/9
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http://dx.doi.org/10.1021/acs.joc.5b01013 |
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Título
Synthetic studies on the preparation of alanyl epoxysulfones as cathepsin cysteine protease electrophilic trapsAutoría
Fecha de publicación
2015-07Editor
American Chemical SocietyCita bibliográfica
LATORRE, Antonio, et al. Synthetic Studies on the Preparation of Alanyl Epoxysulfones as Cathepsin Cysteine Protease Electrophilic Traps. The Journal of organic chemistry, 2015, vol. 80, no 15, p. 7752-7756.Tipo de documento
info:eu-repo/semantics/articleVersión de la editorial
http://pubs.acs.org/doi/abs/10.1021/acs.joc.5b01013Palabras clave / Materias
Resumen
A Darzens reaction between tert-butoxycarbonyl alaninal and chloromethyl phenyl sulfone afforded chlorohydrins, which were converted into epoxysulfones by reaction with sodium tert-butoxide. Epoxysulfone 10 and ... [+]
A Darzens reaction between tert-butoxycarbonyl alaninal and chloromethyl phenyl sulfone afforded chlorohydrins, which were converted into epoxysulfones by reaction with sodium tert-butoxide. Epoxysulfone 10 and chloroketone 14 derived from chlorohydrins by oxidation proved to be inhibitors of cathepsins H, S, and C as determined by competitive activity-based protein profiling. [-]
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J. Org. Chem., 2015, 80 (15)Derechos de acceso
Copyright © 2015, American Chemical Society
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