Quest for Novel Chemical Entities through Incorporation of Silicon in Drug Scaffolds

In order to optimize a lead molecule for further development, bioisosteric replacements are generally adopted as one of the strategies. Silicon appears to be the right choice as a carbon isostere because of the similarity in chemical properties. Silicon can be strategically introduced in a molecule to modulate its druglike properties, providing medicinal chemists with an unconventional strategy for replacing a carbon atom. Silicon can also be introduced to replace other heteroatoms and can act as a surrogate of functional groups such as olefin and amide as well. The present Perspective focuses on the opportunities that silicon incorporation offers in drug discovery, with an emphasis on case studies where…

• CF
  Council for Scientific and Industrial Research, South Africa

  Awards: CSC0109, BSC0124, CSC0108
• DO
  Department of Biotechnology, Ministry of Science and Technology, India

  Award: BT/CRS0046/CRS-02/12