SYNTHESIS AND PRELIMINARY ANTILEUKEMIC STUDIES OF CYCLIC MITOGUAZONE ANALOGS

Analogues of mitoguazone bearing a terminal amidino group as a part of the seven-membered ring of 1,3-diazepine and six-membered ring of pyr imidine were prepared in order to evaluate in vivo antileukemic action towards L1210 leukemia in mice. preliminary pharmacological screening showed that the investigated compounds increase the life span (T/C%) of the treated mice in comparison with the untreated animals. The stro ngest antineoplastic effect was exhibited by compound 8. (C) 1998 Else vier Science S.A. All rights reserved.