Application of sulfoximines in medicinal chemistry from 2013 to 2020

Eur J Med Chem. 2021 Jan 1:209:112885. doi: 10.1016/j.ejmech.2020.112885. Epub 2020 Sep 28.

Abstract

In recent years, interest in sulfoximine chemistry has been greatly increased. For example, at least three sulfoximine containing drugs BAY 1143572, BAY 1251152 and AZD6738 have entered the clinic. Despite the increasing interest in sulfoximines and their chemistry, the routine application of this structure in drug discovery is still hampered due to limited experience in physicochemical and in vitro parameters of sulfoximines. Therefore, we reviewed all relevant articles from 2013 to the present in terms of potency and pharmacokinetic properties in order to support the addition of the sulfoximine component to the toolbox of medicinal chemists.

Keywords: Drug design; Pharmacophore; Sulfoximine.

Publication types

  • Review

MeSH terms

  • Animals
  • Chemistry, Pharmaceutical
  • Drug Development*
  • Drug Discovery*
  • Humans
  • Indoles
  • Morpholines
  • Pyrimidines / chemistry
  • Pyrimidines / pharmacokinetics
  • Pyrimidines / pharmacology
  • Sulfonamides / chemistry
  • Sulfonamides / pharmacokinetics
  • Sulfonamides / pharmacology
  • Sulfoxides / chemistry
  • Sulfoxides / pharmacokinetics
  • Sulfoxides / pharmacology
  • Sulfur Compounds / chemistry*
  • Sulfur Compounds / pharmacokinetics
  • Sulfur Compounds / pharmacology
  • Triazines / chemistry
  • Triazines / pharmacokinetics
  • Triazines / pharmacology

Substances

  • Indoles
  • Morpholines
  • Pyrimidines
  • Sulfonamides
  • Sulfoxides
  • Sulfur Compounds
  • Triazines
  • atuveciclib
  • ceralasertib