Abstract
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.
- Copyright © 1976 by Academic Press, Inc.
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