Issue 8, 2011
From the journal:

Chemical Society Reviews

Boron-containing inhibitors of synthetases†

Stephen J. Baker,*a   John W. Tomshob  and  Stephen J. Benkovicc  

* Corresponding authors

a Anacor Pharmaceuticals, Inc., 1020 E. Meadow Circle, Palo Alto, CA, USA
E-mail: sbaker@anacor.com
Fax: +1 650 543 7660
Tel: +1 650 543 7543

b The Pennsylvania State University, 104 Chemistry Building, Chemistry Department, University Park, PA, USA
E-mail: jwt11@psu.edu
Fax: +1 814 865 2973
Tel: +1 814 865 9508

c The Pennsylvania State University, 414 Wartik Building, Chemistry Department, University Park, PA, USA
E-mail: sjb1@psu.edu
Fax: +1 814 865 2973
Tel: +1 814 865 2882

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 (Velcade®) 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

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Article information

DOI
https://doi.org/10.1039/C0CS00131G
Article type
Tutorial Review
Submitted
01 Oct 2010
Accepted
11 Jan 2011
First published
07 Feb 2011

Chem. Soc. Rev., 2011,40, 4279-4285

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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

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