In order to study a new antitumor
platinum complex, various
platinum complexes were prepared from 2-amino-methylpyrrolidine derivatives synthesized to serve as carrier
ligands and tested for their antitumor activity against Colon 26
carcinoma (s.c.-i.p. system) and
P388 leukemia (i.p.-i.p. system) in mice. 2-Aminomethylpyrrolidine proved to be the most effective carrier
ligand in its
amine derivatives. The structure-activity relationships of the carrier
ligands in the
platinum complexes with dichloro, oxalato, 1,1-cyclobutanedicarboxylato and dichlorodihydroxo as leaving group were clearly shown on the Colon 26
carcinoma screen and were as follows: the antitumor activity of the
platinum complexes with any leaving groups was considerably decreased by the substitution of
hydrogen by alkyl group (Me, Et) on
nitrogen of aminomethyl and the effects of 1,1-cyclobutanedicarboxylato Pt(II) complexes completely disappeared with the same substitution on
nitrogen of
pyrrolidine. In all the tested
platinum complexes 2-aminomethylpyrrolidine(1,1-cyclobutanedicarboxylato)platin um(II) (15) exhibited the most potent antitumor activity. 15 was superior to 1,1-cyclobutanedicarboxylatodiammineplatinum(II) (
CBDCA) and similar to
cis-diamminedichloroplatinum(II) (CDDP) on the Colon 26
carcinoma screen but it was inferior to
CBDCA and CDDP on the
P388 leukemia screen. Furthermore, 15 showed more potent antitumor activity than
CBDCA against Colon 38
carcinoma (s.c.-i.p. system).