Polycyclic Sulfoximines as New Scaffolds for Drug Discovery

被引：22

作者：

Borst, Mark L. G. ^{[1
]}

Ouairy, Cecile M. J. ^{[1
]}

Fokkema, Sander C. ^{[1
]}

Cecchi, Alessandro ^{[1
]}

Kerckhoffs, Jessica M. C. A. ^{[1
]}

de Boer, Vincent L. ^{[1
]}

van den Boogaard, Peter J. ^{[1
]}

Bus, Rutger F. ^{[1
]}

Ebens, Rijko ^{[1
]}

van der Hulst, Rob ^{[1
]}

Knol, Joop ^{[1
]}

Libbers, Rob ^{[1
]}

Lion, Zhou M. ^{[1
]}

Settels, Bart W. ^{[1
]}

de Weyer, Ellen ^{[1
]}

Attia, Khaled A. ^{[1
]}

Sinnema, Piet-Jan ^{[1
]}

de Gooijer, Jesse M. ^{[1
]}

Harkema, Karen ^{[1
]}

Hazewinkel, Marieke ^{[1
]}

Snijder, Susan ^{[1
]}

Pouwer, Kees ^{[1
]}

机构：

[1] Syncom BV, Kadijk 3, NL-9747 AT Groningen, Netherlands

来源：

ACS COMBINATORIAL SCIENCE | 2018年 / 20卷 / 06期

关键词：

sulfoximines; bridged bicyclic structures; bicyclic pyrazoles; heteroatom-substituted Spiro [3.3]heptanes; library production; European Lead Factory; SYNTHETIC STRATEGIES; MEDICINAL CHEMISTRY; KINASE INHIBITOR; PERSPECTIVE; RELEVANT; ANALOGS; CANCER; SPACE; RING;

D O I：

10.1021/acscombsci.7b00150

中图分类号：

O69 [应用化学];

学科分类号：

081704 ;

摘要：

The design and synthesis of three novel polycyclic scaffolds containing sulfoximines are presented in this work, which exemplify that sulfoximines represent a real opportunity for the discovery of new drug candidates. Additionally, the structures present at least two points of diversification and contain a high level of sp(3)-character, hence being very interesting 3D scaffolds. The compounds synthesized were added to the compound collection of the European Lead Factory.

引用

页码：335 / 343

页数：9

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