Synthetic studies on the preparation of alanyl epoxysulfones as cathepsin cysteine protease electrophilic traps
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Altres documents de l'autoria: Latorre, Antonio; Rodríguez, Santiago; González, Florenci; Florea, Bogdan I.; Overkleeft, Herman S.
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Mostra el registre complet de l'elementcomunitat-uji-handle:10234/9
comunitat-uji-handle2:10234/7053
comunitat-uji-handle3:10234/8639
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http://dx.doi.org/10.1021/acs.joc.5b01013 |
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Títol
Synthetic studies on the preparation of alanyl epoxysulfones as cathepsin cysteine protease electrophilic trapsAutoria
Data de publicació
2015-07Editor
American Chemical SocietyCita bibliogràfica
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.Tipus de document
info:eu-repo/semantics/articleVersió de l'editorial
http://pubs.acs.org/doi/abs/10.1021/acs.joc.5b01013Paraules clau / Matèries
Resum
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. [-]
Publicat a
J. Org. Chem., 2015, 80 (15)Drets d'accés
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