Novel Pieces for the Emerging Picture of Sulfoximines in Drug Discovery: Synthesis and Evaluation of Sulfoximine Analogues of Marketed Drugs and Advanced Clinical Candidates

被引：167

作者：

Sirvent, Juan Alberto ^{[1
]}

Luecking, Ulrich ^{[1
]}

机构：

[1] Bayer AG, Drug Discovery, Mullerstr 178, D-13353 Berlin, Germany

来源：

CHEMMEDCHEM | 2017年 / 12卷 / 07期

关键词：

drug design; kinase inhibitors; medicinal chemistry; pharmacophores; sulfoximines; DEPENDENT KINASE INHIBITOR; PHOSPHODIESTERASE-5; INHIBITORS; ASYMMETRIC-SYNTHESIS; CDK4/6; INHIBITOR; POTENT INHIBITOR; STRUCTURAL BASIS; BUILDING-BLOCKS; NH-SULFOXIMINES; ABL PROTEIN; LIGANDS;

D O I：

10.1002/cmdc.201700044

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

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), BAY1143572 (P-TEFb inhibitor), and AZD6738 (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 invitro 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.

引用

页码：487 / 501

页数：15

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