1. Novel Pieces for the Emerging Picture of Sulfoximines in Drug Discovery: Synthesis and Evaluation of Sulfoximine Analogues of Marketed Drugs and Advanced Clinical Candidates.
- Author
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Sirvent JA and Lücking U
- Subjects
- Aminopyridines chemical synthesis, Aminopyridines chemistry, Aminopyridines metabolism, Ataxia Telangiectasia Mutated Proteins antagonists & inhibitors, Ataxia Telangiectasia Mutated Proteins metabolism, Cyclin-Dependent Kinases antagonists & inhibitors, Cyclin-Dependent Kinases metabolism, Estradiol analogs & derivatives, Estradiol chemical synthesis, Estradiol chemistry, Estradiol metabolism, Fulvestrant, Imatinib Mesylate chemical synthesis, Imatinib Mesylate chemistry, Imatinib Mesylate metabolism, Piperazines chemical synthesis, Piperazines chemistry, Piperazines metabolism, Piperidines chemical synthesis, Piperidines chemistry, Piperidines metabolism, Protein Kinase Inhibitors chemical synthesis, Protein Kinase Inhibitors metabolism, Purines chemical synthesis, Purines chemistry, Purines metabolism, Pyrazoles chemical synthesis, Pyrazoles chemistry, Pyrazoles metabolism, Pyridines chemical synthesis, Pyridines chemistry, Pyridines metabolism, Sulfoxides chemical synthesis, Sulfoxides metabolism, Vardenafil Dihydrochloride chemical synthesis, Vardenafil Dihydrochloride chemistry, Vardenafil Dihydrochloride metabolism, Drug Design, Protein Kinase Inhibitors chemistry, Sulfoxides chemistry
- 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., (© 2017 Wiley-VCH Verlag GmbH & Co. KGaA, Weinheim.)
- Published
- 2017
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