Rp. Alexander et al., A N-NITROSOCHLOROETHYL-CEPHALOSPORIN CARBAMATE PRODRUG FOR ANTIBODY-DIRECTED ENZYME PRODRUG THERAPY (ADEPT), Tetrahedron, 52(16), 1996, pp. 5983-5988
N-Nitrosochloroethyl-cephem 7 was prepared via acylation and selective
nitrosation of a cephalothin derivative. This cephalosporin is an eff
icient substrate for Enterobacter cloacae P99 beta-lactamase. Kinetic
parameters were determined for enzyme-catalysed hydrolysis. This cepha
losporin is a potential prodrug for the delivery of bis-alkylating chl
oroethyldiazo species to tumours by antibody-beta-lactamase conjugates
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