Relationship between the structures of taxane derivatives and their microtubule polymerization activity.
Biosci Biotechnol Biochem
; 76(2): 349-52, 2012.
Article
en En
| MEDLINE
| ID: mdl-22313785
ABSTRACT
Paclitaxel (Taxol), one of the most potent anticancer drugs, is a microtubule-stabilizing compound that inhibits microtubule depolymerization within the cell. The structure of paclitaxel is composed of two key elements, a taxane ring and an N-benzoylphenylisoserine side chain at C-13. A number of natural and artificial compounds with taxane skeletons have been isolated, but almost none of their bioactivities have been evaluated. In this study, we focused on compounds having a taxane skeleton structure and examined their effects on tubulin dynamics. Although none of these compounds had an N-benzoylphenylisoserine side chain, three were found to promote tubulin assembly. On the other hand, one compound inhibited tubluin assembly in a way similar to nocodazole. These compounds exhibited novel structure-activity relationships of taxane compounds.
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Colección:
01-internacional
Base de datos:
MEDLINE
Asunto principal:
Hidrocarburos Aromáticos con Puentes
/
Taxoides
/
Microtúbulos
Límite:
Animals
/
Humans
Idioma:
En
Revista:
Biosci Biotechnol Biochem
Asunto de la revista:
BIOQUIMICA
/
BIOTECNOLOGIA
Año:
2012
Tipo del documento:
Article
País de afiliación:
Japón