Boron-containing inhibitors of synthetases

Stephen J. Baker; John W. Tomsho; Stephen J. Benkovic

doi:10.1039/c0cs00131g

Boron-containing inhibitors of synthetases

Stephen J. Baker, John W. Tomsho, Stephen J. Benkovic

Chemistry

Research output: Contribution to journal › Article › peer-review

221 Scopus citations

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.

Original language	English (US)
Pages (from-to)	4279-4285
Number of pages	7
Journal	Chemical Society Reviews
Volume	40
Issue number	8
DOIs	https://doi.org/10.1039/c0cs00131g
State	Published - Jul 14 2011

All Science Journal Classification (ASJC) codes

General Chemistry

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10.1039/c0cs00131g

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abstract = "The use of boron in small-molecule pharmaceuticals is increasing. Boron{\textquoteright}s ubiquitous occurrence in nature and the recent success of a boronic acid drug (Velcade{\textregistered}) 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.",

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Boron-containing inhibitors of synthetases

Abstract

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