Potential peptidic proteasome inhibitors by incorporation of an electrophilic trap based on amino acid derived α-substituted sulfonyl fluorides.
Bioorg Med Chem
; 25(19): 5055-5063, 2017 10 01.
Article
em En
| MEDLINE
| ID: mdl-28734665
ABSTRACT
Peptido sulfonyl fluoride derivatives were designed and synthesized containing a substituent on the alpha position (αPSFs) with respect to the sulfonyl fluoride electrophilic trap. The chemical reactivity of these α-substituted amino sulfonyl fluorides was studied and compared with the previously described ß-substituted amino sulfonyl fluorides in order to get a deeper insight into the importance of the immediate structural environment of the sulfonyl fluoride moiety. Unfortunately, the poor solubility of the resulting αPSFs precluded a proper evaluation of their biological activity.
Palavras-chave
Texto completo:
1
Coleções:
01-internacional
Base de dados:
MEDLINE
Assunto principal:
Ácidos Sulfínicos
/
Desenho de Fármacos
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Peptidomiméticos
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Inibidores de Proteassoma
Limite:
Humans
Idioma:
En
Revista:
Bioorg Med Chem
Ano de publicação:
2017
Tipo de documento:
Article