Synthesis of (-)-dactylolide and 13-desmethylene-(-)-dactylolide and their effects on tubulin.
Org Lett
; 12(10): 2302-5, 2010 May 21.
Article
en En
| MEDLINE
| ID: mdl-20415434
ABSTRACT
An efficient new synthesis has been elaborated for non-natural (-)-dactylolide ((-)-2) and its 13-desmethylene analogue 4, employing a HWE-based macrocyclization approach with beta-keto-phosphonate/aldehyde 19 and the respective 13-desmethylene derivative as the key intermediates. Both (-)-2 and 4 as well as the corresponding C20 alcohols inhibit human cancer cell proliferation with IC(50) values in the sub-micromolar range and induce the polymerization of tubulin in vitro.
Texto completo:
1
Colección:
01-internacional
Base de datos:
MEDLINE
Asunto principal:
Tubulina (Proteína)
/
Compuestos Bicíclicos Heterocíclicos con Puentes
/
Lactonas
Límite:
Humans
Idioma:
En
Revista:
Org Lett
Asunto de la revista:
BIOQUIMICA
Año:
2010
Tipo del documento:
Article
País de afiliación:
Suiza