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Molecular Pharmacology, Vol 12, 1027-1035, Copyright © 1976 by the American Society for Pharmacology and Experimental Therapeutics

Structure-Activity Relationships for Thiolytic Cleavage Rates of Antitumor Drugs in the 4'-(9-Acridinylamino) methanesulfonanilide Series

BRUCE F. CAIN 1, WILLIAM ROBERT WILSON 1, and BRUCE C. BAGULEY 1

1 Cancer Chemotherapy Laboratory, P. O. Box 1724, Auckland, New Zealand, and Department of Cell Biology, University of Auckland, Auckland, New Zealand

4'-(9-Acridinylamino)methanesulfon-m-anisidide (NSC 156303; m-AMSA) is an experimental broad-spectrum antitumor agent also displaying immunosuppressive and antiviral activity. In pharmacological studies this compound had a short half-life in vivo as a result of rapid chemical reaction with proteins. Interaction of m-AMSA with thiols and other nucleophiles has been studied and the reaction products characterized. The reaction of greatest biological relevance is nucleophilic attack at the acridine C-9 position by thiols. The relationships among structure, thiolysis rates, and antileukemic activity of over 50 substituted acridines have been investigated. Rapid reaction with thiols is not a prerequisite for antileukemic (L1210) activity with these agents.

Submitted on March 2, 1976
Accepted on July 6, 1976






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