Synthesis and antitumor activities of platinum complexes of unsymmetrical alicyclic diamines as carrier ligands.
The synthesis and biological activities of the platinum complexes of 2-aminomethylaziridine, 2-aminomethylazetidine, 2-aminomethylpyrrolidine, 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)platin um 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.
Morikawa
K
K
Exploratory Research Laboratories, Chugai Pharmaceutical Company, Ltd., Gotemba-shi, Japan.
Honda
M
M
Endoh
K
K
Matsumoto
T
T
Akamatsu
K
K
Mitsui
H
H
Koizumi
M
M
D000818:Animals; D000970:Antineoplastic Agents / Q000138:chemical synthesis*; D002277:Carcinoma / Q000188:drug therapy; D003110:Colonic Neoplasms / Q000188:drug therapy; D003959:Diamines / Q000138:chemical synthesis* / Q000494:pharmacology; D004337:Drug Carriers; D007941:Leukemia P388 / Q000188:drug therapy; D008024:Ligands; D008297:Male; D051379:Mice; D008815:Mice, Inbred Strains; D009944:Organoplatinum Compounds / Q000138:chemical synthesis*
D000970:Antineoplastic Agents; D003959:Diamines; D004337:Drug Carriers; D008024:Ligands; D009944:Organoplatinum Compounds