Sulfoximines as Rising Stars in Modern Drug Discovery? Current Status and Perspective on an Emerging Functional Group in Medicinal Chemistry

J Med Chem. 2020 Dec 10;63(23):14243-14275. doi: 10.1021/acs.jmedchem.0c00960. Epub 2020 Sep 23.


Sulfoximines have been largely disregarded in medicinal chemistry for a long time. However, recently, they have risen to the apparent level of stardom on the drug discovery scene. Considering the outstanding properties of sulfoximines, this versatile functional group has advanced to implementation in several drug discovery programs. Currently, this fashionable functional group can be found in various hit-to-lead and lead optimization studies in early stages and in several compounds currently in clinical trials. Herein, we review recent developments to demonstrate the scope and limitations of this interesting and versatile functional group in medicinal chemistry and drug discovery.

MeSH terms

  • Chemistry, Pharmaceutical
  • Drug Discovery*
  • Imines / chemistry*
  • Imines / pharmacology*
  • Sulfur / chemistry*


  • Imines
  • Sulfur