Despite the impressive antitumor activity of
cisplatin, two major limitations of the
drug, that is severe side effects and drug-resistance of
cancer cells, make its use difficult for
cancer therapy. These limitations have resulted in a great deal of effort having been expended into structural modifications of
cisplatin. In this study, we tested two novel
cisplatin analogues, (CPA)2Pt [DOLYM] (COMP-I) and (
DACH)Pt[DOLYM] (COMP-II), for the mode of cytotoxic action against human
tumor cells comparing with
cisplatin and
carboplatin in vitro. These two novel analogues had considerable cytotoxic activities against five kinds of human solid
tumor cells, and especially COMP-II was more effective on HCT15
colon cancer cells than other compounds. In addition, COMP-II had
cytostatic activity at low concentrations (10-0.3 microgram/ml), but other compounds revealed little effect on
tumor growth at the low concentration.