Effects of C7 substitutions in a high affinity microtubule-binding taxane on antitumor activity and drug transport.
Bioorg Med Chem Lett
; 21(16): 4852-6, 2011 Aug 15.
Article
em En
| MEDLINE
| ID: mdl-21764308
ABSTRACT
Some C-7 modified analogs of 3, a taxane with high affinity for binding to microtubules, were prepared through multistep transformations. Most of the analogs, bearing less lipophilic C-7 substituents than propionyl in 3, exhibited comparable binding affinities to microtubules but less cytotoxicity against drug-sensitive as well as multidrug-resistant tumor cells overexpressing P-glycoprotein. In addition, these C7 modifications increased P-glycoprotein-mediated drug transport in both directions in a Caco-2 cell assay.
Texto completo:
1
Coleções:
01-internacional
Base de dados:
MEDLINE
Assunto principal:
Hidrocarbonetos Aromáticos com Pontes
/
Sistemas de Liberação de Medicamentos
/
Taxoides
/
Microtúbulos
/
Antineoplásicos
Limite:
Humans
Idioma:
En
Ano de publicação:
2011
Tipo de documento:
Article