Synthesis and Evaluation of the Anticancer and Trypanocidal Activities of Boronic Tyrphostins.
ChemMedChem
; 13(14): 1395-1404, 2018 07 18.
Article
em En
| MEDLINE
| ID: mdl-29856519
ABSTRACT
Molecules containing an (cyanovinyl)arene moiety are known as tyrphostins because of their ability to inhibit proteins from the tyrosine kinase family, an interesting target for the development of anticancer and trypanocidal drugs. In the present work, (E)-(cyanovinyl)benzeneboronic acids were synthesized by Knoevenagel condensations without the use of any catalysts in water through a simple protocol that completely avoided the use of organic solvents in the synthesis and workup process. The inâ
vitro anticancer and trypanocidal activities of the synthesized boronic acids were also evaluated, and it was discovered that the introduction of the boronic acid functionality improved the activity of the boronic tyrphostins. Inâ
silico target fishing with the use of a chemogenomic approach suggested that tyrosine-phosphorylation-regulated kinaseâ
1a (DYRK1A) was a potential target for some of the designed compounds.
Palavras-chave
Texto completo:
1
Bases de dados:
MEDLINE
Assunto principal:
Tripanossomicidas
/
Compostos de Boro
/
Tirfostinas
/
Antineoplásicos
Limite:
Animals
/
Humans
Idioma:
En
Revista:
ChemMedChem
Assunto da revista:
FARMACOLOGIA
/
QUIMICA
Ano de publicação:
2018
Tipo de documento:
Article
País de afiliação:
Brasil