Phenyl sulfur mustard derivatives of distamycin A

Bioorganic & Medicinal Chemistry Letters
2000.0

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-derived cytotoxics, about 1000 times more potent than melphalan.

Knowledge Graph

Similar Paper

Phenyl sulfur mustard derivatives of distamycin A
Bioorganic & Medicinal Chemistry Letters 2000.0
Synthesis and Antitumor Activity of New Benzoheterocyclic Derivatives of Distamycin A
Journal of Medicinal Chemistry 2000.0
Synthesis, DNA-binding properties, and antitumor activity of novel distamycin derivatives
Journal of Medicinal Chemistry 1989.0
In vitro cytotoxicity of GC sequence directed alkylating agents related to distamycin
Journal of Medicinal Chemistry 1993.0
Synthesis, structure–activity relationship and biological evaluation of novel nitrogen mustard sophoridinic acid derivatives as potential anticancer agents
Bioorganic & Medicinal Chemistry Letters 2015.0
Synthesis and biological activity of stable and potent antitumor agents, aniline nitrogen mustards linked to 9-anilinoacridines via a urea linkage
Bioorganic & Medicinal Chemistry 2008.0
Design, synthesis and potent cytotoxic activity of novel 7-( N -[(substituted-sulfonyl)piperazinyl]-methyl)-camptothecin derivatives
Bioorganic & Medicinal Chemistry Letters 2017.0
The synthesis and biological evaluation of new DNA-directed alkylating agents, phenyl N-mustard-4-anilinoquinoline conjugates containing a urea linker
European Journal of Medicinal Chemistry 2014.0
Derivatives of aryl amines containing the cytotoxic 1,4-dioxo-2-butenyl pharmacophore
Bioorganic & Medicinal Chemistry Letters 2010.0
Synthesis, in vitro antimicrobial and cytotoxic activities of novel pyrimidine–benzimidazol combinations
Bioorganic & Medicinal Chemistry Letters 2014.0