Synthesis of isotopically labeled epothilones.
J Labelled Comp Radiopharm
; 57(2): 78-81, 2014 Feb.
Article
en En
| MEDLINE
| ID: mdl-24307484
ABSTRACT
The epothilones, including epothilones B and D, are macrocyclic lactones, which have potent cytotoxicities and promote the polymerization of tubulin to mictotubules by binding to and stabilizing the tubulin polymer. They have a very similar mechanism of action to paclitaxel (Taxol®). The determination of the microtubule-binding conformation of the epothilones is an important piece of information in designing improved analogs for possible clinical use, and internuclear distance information that will assist the determination of this conformation can be obtained by rotational echo double resonance (REDOR) NMR studies of microtubule-bound epothilones with appropriate stable isotope labels. Analogs of epothilone B and epothilone D with [(2) H3 ] and [(19) F] labels were prepared from an advanced precursor for potential use in REDOR NMR studies to determine internuclear distances in tubulin-bound ligand.
Palabras clave
Texto completo:
1
Colección:
01-internacional
Base de datos:
MEDLINE
Asunto principal:
Epotilonas
/
Deuterio
/
Moduladores de Tubulina
/
Marcaje Isotópico
Límite:
Humans
Idioma:
En
Revista:
J Labelled Comp Radiopharm
Año:
2014
Tipo del documento:
Article
País de afiliación:
Estados Unidos