Design and synthesis of a beta-lactamase activated 5-fluorouracil prodrug.
Bioorg Med Chem Lett
; 19(4): 1261-3, 2009 Feb 15.
Article
em En
| MEDLINE
| ID: mdl-19167216
ABSTRACT
An efficient synthesis of a 5-fluorouracil-cephalosporin prodrug is described for use against colorectal and other cancers in antibody and gene-directed therapies. The compound shows stability in aqueous media until specifically activated by beta-lactamase (betaL). The kinetic parameters of the 5-fluorouracil-cephalosporin conjugate were determined in the presence of Enterobacter cloacae P99 betaL (ECl betaL) revealing a K(m)=95.4 microM and V(max)=3.21 microMol min(-1) mg(-1). The data compare favorably to related systems that have been reported and enable testing of this prodrug against cancer cell lines in vitro and in vivo.
Texto completo:
1
Base de dados:
MEDLINE
Assunto principal:
Beta-Lactamases
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Pró-Fármacos
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Enterobacter cloacae
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Fluoruracila
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Antineoplásicos
Idioma:
En
Revista:
Bioorg Med Chem Lett
Assunto da revista:
BIOQUIMICA
/
QUIMICA
Ano de publicação:
2009
Tipo de documento:
Article
País de afiliação:
Estados Unidos