Synthesis and antitumor activity of 1,2-diaminocyclohexane platinum(IV) complexes (original) (raw)

1994, Journal of Inorganic Biochemistry

The synthesis, characterization, and antitumor activity of a series of platinum(IV) complexes of the type DACH-Pt'"(X),Y (where DACH = truns-dl, or buns-1-1,2-diaminocyclohexane, X = OH or Cl, and Y = oxalato, malonato, methylmalonato, tartronato, ketomalonato, l,l-cyclopropanedicarboxylato, or l,l-cyclobutanedicarbor@ato, are described. These complexes have been characterized by elemental analysis, HPLC, and infrared and '95Pt NMR spectroscopic techniques. The complexes had good in vitro cytotoxic activity (IC,, = 0.14-7.6 pg/ml) and were highly active in vivo against leukemia L1210 cells (%T/C = 152-> 600, cisplatin = 218). In addition, excellent in vivo antitumor activities against B16 melanoma (%T/C = 309), M.5076 reticulosarcoma (100% cures) and cisplatin-resistant Ll%lO/DDP (%T/C = 217) cell lines were also exhibited by an analog selected for further evaluation.