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Curr Opin Drug Discov Devel. 2007 Nov;10(6):654-71.

The synthesis of biologically active organosilicon small molecules.

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  • 1Department of Chemistry, University of California, Davis, CA 95616, USA.


The biological investigation of organosilicon small molecules is of particular interest as the addition of silicon to small molecules can alter their chemical properties, enhancing biological activity and improving pharmacological profiles. Although silicon is often only employed as a transient component to promote stereoselective synthesis or to provide a reactive functional handle, recent reports have demonstrated that organosilicon small molecules can undergo potent and selective interactions with biological macromolecules and have enhanced activity in cellular assays. This review summarizes developments in the synthesis and study of biologically active organosilicon small molecules, including stability and reactivity studies that are relevant to synthetic methodology and medicinal chemistry. The stereoselective synthesis of diverse silyl-functionalized heterocycles is also discussed, compounds which could potentially display interesting and novel biological activity.

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