Design, synthesis and structure-activity relationships of novel taxane-based multidrug resistance reversal agents.
J Med Chem
; 48(6): 2218-28, 2005 Mar 24.
Article
em En
| MEDLINE
| ID: mdl-15771464
ABSTRACT
A series of novel taxane-based multidrug resistance (MDR) reversal agents (TRAs) has been designed and synthesized. Structure-activity relationship (SAR) study clearly indicates that modification of the C-7 position with hydrophobic arenecarbonylcinnamoyl groups brings about high potency against drug efflux mediated by P-glycoprotein (P-gp). Six TRAs exhibit ability to modulate a wide range of ATP-binding cassette (ABC) transporters, such as P-gp, multidrug resistance-associated protein 1 (MRP1), and breast cancer resistance protein (BCRP), which may serve as novel broad-spectrum modulators of ABC transporters.
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Coleções:
01-internacional
Base de dados:
MEDLINE
Assunto principal:
Resistência a Múltiplos Medicamentos
/
Resistencia a Medicamentos Antineoplásicos
/
Taxoides
/
Antineoplásicos
Limite:
Humans
Idioma:
En
Ano de publicação:
2005
Tipo de documento:
Article