Thiol-dependent DNA cleavage by aminomethylated Beaucage's reagent?

Organic & Biomolecular Chemistry Pub Date: 2010-02-03 DOI: 10.1039/B926217B

Abstract

Aminomethylated Beaucage's reagent 1 was found to be more potent than 3H-1,2-benzodithiol-3-one 1,1-dioxide (Beaucage's reagent) in causing DNA cleavage. The current study demonstrated the importance of the amino functionality in enhancing DNA-cleaving activities, and such findings may facilitate development of novel sulfur-containing DNA-cleaving molecules in cancer therapy.

Graphical abstract: Thiol-dependent DNA cleavage by aminomethylated Beaucage's reagent
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