Synthesis and antitumor activities of platinum complexes of unsymmetrical alicyclic diamines as carrier ligands

Abstract

The synthesis and biological activities of the platinum complexes of 2‐aminomethylaziridine, 2‐aminomethylazetidine, 2‐aminomethylpyrrolidine, and 2‐aminomethylpiperidine as carrier ligands are described. The platinum complexes of 2‐aminomethylazetidine and 2‐aminomethylpyrrolidine are significantly effective against murine tumors. In particular, 2‐aminomethylazetidine(1, 1‐cyclobutanedicarboxylato)platinum II (13) and 2‐aminomethylpyrrolidine(1, 1‐cyclobutanedicarboxylato)platinum II (16) exhibited potent antitumor activity and were soluble in water, and their antitumor activities against Colon 26 carcinoma (sc‐ip system) were superior to CBDCA and comparable to CDDP. Copyright © 1990 Wiley‐Liss, Inc., A Wiley Company