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Issue 8, 2011
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Boron-containing inhibitors of synthetases†

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

* 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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Publication details

The article was received on 01 Oct 2010, accepted on 11 Jan 2011 and first published on 07 Feb 2011


Article type: Tutorial Review
DOI: 10.1039/C0CS00131G
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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