title: Progress in the medicinal chemistry of silicon: C/Si exchange and beyond.
abstract: Application of silyl functionalities is one of the most promising strategies among various 'elements chemistry' approaches for the development of novel and distinctive drug candidates. Replacement of one or more carbon atoms of various biologically active compounds with silicon (so-called sila-substitution) has been intensively studied for decades, and is often effective for alteration of activity profile and improvement of metabolic profile. In addition to simple C/Si exchange, several novel approaches for utilizing silicon in medicinal chemistry have been suggested in recent years, focusing on the intrinsic differences between silicon and carbon. Sila-substitution offers great potential for enlarging the chemical space of medicinal chemistry, and provides many options for structural development of drug candidates.
authors.affiliation: Institute of Molecular and Cellular Biosciences, The University of Tokyo, 1-1-1 Yayoi, Bunkyo-ku, Tokyo 113-0032, Japan.
authors.forename: Shinya
authors.initials: S
authors.lastname: Fujii
authors.affiliation: Institute of Molecular and Cellular Biosciences, The University of Tokyo, 1-1-1 Yayoi, Bunkyo-ku, Tokyo 113-0032, Japan.
authors.forename: Yuichi
authors.initials: Y
authors.lastname: Hashimoto
mesh_terms: D002244:Carbon / Q000737:chemistry*; D002626:Chemistry, Pharmaceutical / Q000639:trends*; D006801:Humans; D015394:Molecular Structure; D012825:Silicon / Q000737:chemistry*
chemical_list: D002244:Carbon; D012825:Silicon
keywords: C/Si-exchange; elements chemistry; heavier group 14 elements; isosterism; sila-drug; sila-substitution; silicon