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Bioorg. Med. Chem. Lett. · Feb 2009
Design and synthesis of a beta-lactamase activated 5-fluorouracil prodrug.
- Ryan M Phelan, Marc Ostermeier, and Craig A Townsend.
- Department of Chemistry, Johns Hopkins University, 3400 N. Charles St., Baltimore, MD 21212, USA.
- Bioorg. Med. Chem. Lett. 2009 Feb 15; 19 (4): 1261-3.
AbstractAn 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.
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