NOVEL PHENYL NITROGEN-MUSTARD AND HALF-MUSTARD DERIVATIVES OF AMIDINO-MODIFIED DISTAMYCIN

The design, synthesis, and in vitro and in vivo activities of novel be nzoyl and cinnamoyl nitrogen mustard and half-mustard derivatives of d istamycin A, in which the amidino moiety has been replaced by moieties of different physico-chemical features, are described and structure-a ctivity relationships are discussed. Some amidino-modified derivatives show significant cytotoxicity and antileukemic activity. (C) 1997 Els evier Science Ltd.