NEW ANTITUMOR PLATINUM(II) COMPLEXES WITH BOTH LIPOPHILICITY AND WATER MISCIBILITY

Water‐miscible platinum(II) complexes with 1,2‐diaminocyclohexane as the carrier ligand and bile acids as the leaving ligands were synthesized and tested for antitumor activity against intra‐peritoneally implanted leukemia L1210 cells in mice. These complexes were water‐miscible after appropriate sonication due to the presence of hydrophilic hydroxyl groups in the molecule, even though the complexes were essentially lipophilic. The complexes had high antitumor activity, but their optimal dose levels differed, and the administration route and form affected the antitumor activity. More lipophilic complexes showed higher activity when administered with Lipiodol than in water suspension, while the hydrophilic complexes showed significant activity when administered in water suspension. Intravenous administration of DACHP(cheno)2 in water suspension resulted in potent antitumor activity, while other complexes showed moderate activity via this route. Copyright © 1990, Wiley Blackwell. All rights reserved