Novel Phenyl Nitrogen Mustard and Half-Mustard Derivatives of Amidino-Modified Distamycin.

Abstract The design, synthesis, and in vitro and in vivo activities of novel benzoyl and cinnamoyl nitrogen mustard and half-mustard derivatives of distamycin A, in which the amidino moiety has been replaced by moieties of different physico-chemical features, are described and structure-activity relationships are discussed. Some amidino-modified derivatives show significant cytotoxicity and antileukemic activity.