TUMOR INHIBITORY EFFECT OF A NEW SERIES OF METHANESULFONATE OF AMINOGLYCOLS

Abstract

The antitumor activities of nine new methanesulfonates of aminoglycols were evaluated. Two compounds, 3, 3'-(morpholinopropylimino)-di(1-propanol) dimethanesulfonate (ester) dihydrochloride (No. 888) and 3, 3'-(dibutylaminopropylimino)-di(1-propanol) dimethanesulfonate (ester) dihydroehloride (No. 893), showed marked activities against rats bearing Yoshida sarcoma. These two compounds cured 70-80% of the treated rats at their optimal doses. On the ascites hepatomas, when the tumor was inoculated intraperitoneally and the drug was given by the same route, 3, 3'-(methylimino)-di(1-propanol) dimethanesulfonate (ester) diphenyldisulfonate (No. 838D) was better than No. 888 or 893. However, when the tumor was intravenously inoculated and the drug was intraperitoneally given, or when the tumor was intravenously inoculated and the drug was given by the same route, a clear difference in their activities was observed. No. 838D was the most active against AH-272 and Nos. 888 and 893 against AH-66, but No. 893 was less active than No. 888.