Novel Pieces for the Emerging Picture of Sulfoximines in Drug Discovery: Synthesis and Evaluation of Sulfoximine Analogues of Marketed Drugs and Advanced Clinical Candidates. (22nd March 2017)

• Record Type: Journal Article
• Authors: Sirvent, Juan Alberto; Lücking, Ulrich
• Is Part Of: ChemMedChem. Volume 12:Number 7(2017)
• Page Start: 487
• Page End: 501
• Publication Date: 2017-03-22
• Subjects: drug design -- kinase inhibitors -- medicinal chemistry -- pharmacophores -- sulfoximines; Pharmaceutical chemistry -- Periodicals; 615.19005
• DOI: 10.1002/cmdc.201700044
• Languages: English
• ISSNs: 1860-7179

Abstract

Abstract: Sulfoximines have gained considerable recognition as an important structural motif in drug discovery of late. In particular, the clinical kinase inhibitors for the treatment of cancer, roniciclib (pan‐CDK inhibitor), BAY 1143572 (P‐TEFb inhibitor), and AZD 6738 (ATR inhibitor), have recently drawn considerable attention. Whilst the interest in this underrepresented functional group in drug discovery is clearly on the rise, there remains an incomplete understanding of the medicinal‐chemistry‐relevant properties of sulfoximines. Herein we report the synthesis and in vitro characterization of a variety of sulfoximine analogues of marketed drugs and advanced clinical candidates to gain a better understanding of this neglected functional group and its potential in drug discovery. Abstract : The long‐neglected sulfoximine group has recently enjoyed a rapidly increasing interest in the life sciences. The synthetic methodology for sulfoximines has progressed over the last decade; however, the general understanding of this functional group regarding is medicinal‐chemistry‐relevant properties is limited. We report the synthesis and in vitro characterization of six sulfoximine analogues of marketed drugs and clinical candidates.