Synthesis, Characterization, and Bioactivity of the Photoisomerizable Tubulin Polymerization Inhibitor azo-Combretastatin A4.
Org Lett
; 17(18): 4546-9, 2015 Sep 18.
Article
em En
| MEDLINE
| ID: mdl-26335519
ABSTRACT
Combretastatin A4 is a stilbenoid tubulin binding mitotic inhibitor whose conformation greatly influences its potency, making it an excellent candidate for adaptation as a photoactivatable tool. Herein we report a novel synthesis, the facile isomerization with commercial grade equipment, and biological activity of azo-combretastatin A4 in vitro and in human cancer cells. Photoisomerized azo-combretestatin A4 is at least 200-fold more potent in cellular culture, making it a promising phototherapeutic and biomedical research tool.
Texto completo:
1
Coleções:
01-internacional
Base de dados:
MEDLINE
Assunto principal:
Estilbenos
/
Moduladores de Tubulina
Limite:
Humans
Idioma:
En
Revista:
Org Lett
Ano de publicação:
2015
Tipo de documento:
Article