Syntheses and evaluation of novel fatty acid-second-generation taxoid conjugates as promising anticancer agents.
Bioorg Med Chem Lett
; 16(4): 974-7, 2006 Feb 15.
Article
em En
| MEDLINE
| ID: mdl-16298526
ABSTRACT
Polyunsaturated fatty acids such as docosahexaenoic acid (DHA), linolenic acid, and linoleic acid were linked to the C-2' position of the second-generation taxoids that could overcome MDR caused by overexpressed ABC transporters. The new conjugates, tested in vivo, exhibited strong activity against drug-resistant colon cancer and drug-sensitive ovarian cancer xenografts in mice. Two of the new conjugates, DHA-SB-T-1214 and DHA-SB-T-1213, were found to achieve the total regression of drug-resistant and drug-sensitive tumors, respectively, in the animal models with substantially reduced systemic toxicity.
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Base de dados:
MEDLINE
Assunto principal:
Taxoides
/
Ácidos Graxos Insaturados
/
Antineoplásicos
Idioma:
En
Ano de publicação:
2006
Tipo de documento:
Article