NEW MATERIAL:The compound of formula I {A is residue formed by removing N-terminal amino group and C-terminal carboxyl group from a dipeptide or tripeptide composed of α-amino acids; R1 is amino or methoxy; one of R2 and R3 is R4CO- [R4 is H, (substituted) lower alkyl, cycloalkyl, (substituted) aryl, etc.], R4OCO-, R4SO2-, R4NHCO-, etc., and the other is H or both groups together form group of formula II (R6 is arylene)}.
EXAMPLE: 1a-(tert-Butyloxycarbonyl-L-alanyl-L-prolyl)mitomycin C.
USE: A medicine. An antitumor agent. it is administered at a dose of 2W150mg of the active component per 60kg body weight daily.
PREPARATION: The compound of formula I can be produced by condensing mitomycin C of formula III (R1 is NH2) or mitomycin A (A1 is OCH3) with the compound of formula IV in an inert solvent in the presence of a coupling reagent at a temperature between 0°C and room temperature for several W 24hr.
KURODA TOKUYUKI
MORIMOTO MAKOTO
