HYPOXIA-SELECTIVE ANTITUMOR AGENTS DERIVED FROM 1,9-DIAZAANTHRACENE

The nitroacridine derivative [3-(N,N-dimethylamino)propylamino]-1-nitr oacridine (nitracrine) is a potent hypoxia-selective cytotoxin for tum or cells in culture. Modifications of the acridine ring result in alte red DNA binding properties. This has suggested the possibility of prep aring new nitracrine analogues retaining the nitro group and the alkyl amino lateral chain. In this paper we describe the synthesis of the ne w diazaanthracenes 4, 5, 6 in order to study the relationships between the heterocyclic system and the hypoxia-selective cytotoxicity. This class of new bioreductive agents may constitute a group of potential i nterest for the design of new cytotoxins.