Halogen-substituted catechol bisphosphates are potent and selective inhibitors of the transcription factor STAT5b.
Bioorg Med Chem
; 25(14): 3871-3882, 2017 07 15.
Article
em En
| MEDLINE
| ID: mdl-28559059
ABSTRACT
The transcription factor STAT5b is an antitumor target. Recently, we presented the small molecules Stafib-1 and Stafib-2 as potent, selective inhibitors of the STAT5b SH2 domain. Here we report that halogen substitutions on the terminal phenyl ring of Stafib-1 and a close derivative are tolerated and specificity over the STAT5a SH2 domain is maintained, albeit with a slight reduction in activity. Our data demonstrate that the synthetic methodology used for generating Stafib-1 and Stafib-2 can be utilized to synthesize a small library of halogen-substituted derivatives, and extend the panel of catechol bisphosphate-based submicromolar and selective STAT5b inhibitors.
Palavras-chave
Texto completo:
1
Bases de dados:
MEDLINE
Assunto principal:
Catecóis
/
Difosfatos
/
Fator de Transcrição STAT5
/
Halogênios
Limite:
Humans
Idioma:
En
Revista:
Bioorg Med Chem
Assunto da revista:
BIOQUIMICA
/
QUIMICA
Ano de publicação:
2017
Tipo de documento:
Article
País de afiliação:
Alemanha