Boron as a platform for new drug design

Expert Opin Drug Discov. 2012 Nov;7(11):1017-27. doi: 10.1517/17460441.2012.717530. Epub 2012 Sep 5.

Abstract

Introduction: Boron lies on the borderline between metals and non-metals in the periodic table. As such, it possesses peculiarities which render it suitable for a variety of applications in chemistry, technology and medicine. However, boron's peculiarities have been exploited only partially so far.

Areas covered: In this review, the authors highlight selected areas of research which have witnessed new uses of boron compounds in recent times. The examples reported illustrate how difficulties in the synthesis and physicochemical characterization of boronated molecules, encountered in past years, can be overcome with positive effects in different fields.

Expert opinion: Many potentialities of boron-based systems reside in the peculiar properties of both boron atoms (the ability to replace carbon atoms, electron deficiency) and of boronated compounds (hydrophobicity, lipophilicity, versatile stereochemistry). Taken in conjunction, these properties can provide innovative drugs. The authors highlight the need to further investigate the assembly of boronated compounds, in terms of drug design, since the mechanisms required to obtain supramolecular structures may be unconventional compared with the more standard molecules used. Furthermore, the authors propose that computational methods are a valuable tool for assessing the role of multicenter, quasi-aromatic bonds and its peculiar geometries.

Publication types

  • Research Support, Non-U.S. Gov't
  • Review

MeSH terms

  • Biocompatible Materials
  • Boron / chemistry*
  • Boron / pharmacology*
  • Drug Delivery Systems
  • Drug Design*
  • Gene Transfer Techniques
  • Nanotubes

Substances

  • Biocompatible Materials
  • Boron