Straightforward access to bisbenzamidine DNA binders and their use as versatile adaptors for DNA-promoted processes?

Chemical Science Pub Date: 2012-05-01 DOI: 10.1039/C2SC00027J

Abstract

Bisbenzamidines are an important family of minor groove DNA-binding agents. We present a one-step synthesis of aromatic aza-bisbenzamidines that allows straightforward and versatile access to a large number of these molecules. One of them, the azide-aza-bisbenzamidine 13, can be readily modified via click-chemistry with a variety of functionalities that can, therefore, be delivered to the vicinity of an A/T-rich DNA minor groove. This strategy, therefore, provides a simple means for triggering site selective, DNA-promoted biochemical and physicochemical processes.

Graphical abstract: Straightforward access to bisbenzamidine DNA binders and their use as versatile adaptors for DNA-promoted processes
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