Jump to main content
Jump to site search

Issue 8, 2011
Previous Article Next Article

Boron-containing inhibitors of synthetases

Author affiliations

Abstract

The use of boron in small-molecule pharmaceuticals is increasing. Boron's ubiquitous occurrence in nature and the recent success of a boronic acid drug (VelcadeĀ®) in the clinic have alleviated many concerns over its use in pharmaceuticals. In addition, the unique physicochemical properties of boronic acids make them an attractive addition to the medicinal chemists toolbox. This tutorial review will discuss these properties and potential benefits for anyone interested in finding novel enzyme inhibitors. An exceptional class of boronic acids, the oxaboroles, will be highlighted and their properties and uses will be discussed in detail. Finally, the current paradigm for the reaction of boronic acids with enzyme nucleophiles will be summarized.

Graphical abstract: Boron-containing inhibitors of synthetases

Back to tab navigation

Article information


Submitted
01 Oct 2010
Accepted
11 Jan 2011
First published
07 Feb 2011

Chem. Soc. Rev., 2011,40, 4279-4285
Article type
Tutorial Review

Boron-containing inhibitors of synthetases

S. J. Baker, J. W. Tomsho and S. J. Benkovic, Chem. Soc. Rev., 2011, 40, 4279
DOI: 10.1039/C0CS00131G

Social activity

Search articles by author

Spotlight

Advertisements