Boron provides some unique chemical properties to small molecules that can be exploited for drug discovery, and over the last decade, pioneering research has demonstrated boron's potential in therapeutic areas including cancer, infectious diseases and inflammation.The electrophilic, empty p orbital, the Lewis acidity, and boron bond lengths provide chemists with the ability to inhibit different targets using a host of different binding modes. Current research is now uncovering how chemists can optimize some of these properties.Boron therapeutics have demonstrated predictable pharmacokinetics and metabolism, and have proven to be similar to other small molecule programs in their safety profiles. As more boron therapeutics advance through clinical trials, and as we learn more about the abilities of these molecule, they are likely to become commonplace in future medicinal chemistry programs.This presentation will review Anacor's experience researching and developing boron-containing small molecules including chemistry, pharmacokinetics, metabolism, safety and clinical studies.

Boron in drug discovery

245th National Meeting (2013)

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