Phenyl sulfur mustard derivatives of distamycin A

The design, synthesis, and cytotoxic activity of novel benzoyl and cinnamoy l sulfur mustard derivatives of distamycin A are described and structure-ac tivity relationships are discussed. These sulfur mustards are more potent c ytotoxics than corresponding nitrogen mustards in spite of the lower alkyla ting power, while their sulfoxide analogues are substantially inactive. Cin namoyl sulfur mustard derivative (7) proved to be one of the most active di stamycin-derived cytotoxics, about 1000 times more potent than melphalan. ( C) 2000 Elsevier Science Ltd. All rights reserved.