Phenyl sulfur mustard derivatives of distamycin A

…, M Caldarelli, L Capolongo, C Geroni, S Mazzini…

Index: Cozzi, Paolo; Beria, Italo; Caldarelli, Marina; Capolongo, Laura; Geroni, Cristina; Mazzini, Stefania; Ragg, Enzio Bioorganic and Medicinal Chemistry Letters, 2000 , vol. 10, # 15 p. 1653 - 1656

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Citation Number: 16

Abstract

The design, synthesis, and cytotoxic activity of novel benzoyl and cinnamoyl sulfur mustard derivatives of distamycin A are described and structure–activity relationships are discussed. These sulfur mustards are more potent cytotoxics than corresponding nitrogen mustards in spite of the lower alkylating power, while their sulfoxide analogues are substantially inactive. Cinnamoyl sulfur mustard derivative (7) proved to be one of the most active distamycin- ...