Cytotoxicity of two novel cisplatin analogues, (CPA)2Pt[DOLYM] and (DACH)Pt[DOLYM], to human cancer cells in vitro.
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.
Choi
S U
SU
Pharmaceutical Screening Lab., Korea Research Institute of Chemical Technology, Taejeon, Korea.
Kim
K H
KH
Choi
E J
EJ
Park
S H
SH
Kim
K M
KM
Shon
Y S
YS
Lee
C O
CO
D000970:Antineoplastic Agents / Q000494:pharmacology*; D016190:Carboplatin / Q000494:pharmacology; D002455:Cell Division / Q000187:drug effects; D002945:Cisplatin / Q000031:analogs & derivatives* / Q000494:pharmacology; D006801:Humans; D009944:Organoplatinum Compounds / Q000494:pharmacology*; D014407:Tumor Cells, Cultured
C119613:(1,2-diaminocyclohexane)(1,3-dithio-2-ylidenemalonate)platinum(II); D000970:Antineoplastic Agents; D009944:Organoplatinum Compounds; C087099:platinum(II) bis(cyclopropylamine)-1,3-dithiol-2-ylidenemalonate; D016190:Carboplatin; D002945:Cisplatin