Polycyclic Sulfoximines as New Scaffolds for Drug Discovery,ACS Combinatorial Science

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Polycyclic Sulfoximines as New Scaffolds for Drug Discovery
ACS Combinatorial Science Pub Date : 2018-05-01 00:00:00 , DOI: 10.1021/acscombsci.7b00150
Mark L. G. Borst ₁ , Cécile M. J. Ouairy ₁ , Sander C. Fokkema ₁ , Alessandro Cecchi ₁ , Jessica M. C. A. Kerckhoffs ₁ , Vincent L. de Boer ₁ , Peter J. van den Boogaard ₁ , Rutger F. Bus ₁ , Rijko Ebens ₁ , Rob van der Hulst ₁ , Joop Knol ₁ , Rob Libbers ₁ , Zhou M. Lion ₁ , Bart W. Settels ₁ , Ellen de Wever ₁ , Khaled A. Attia ₁ , Piet-Jan Sinnema ₁ , Jesse M. de Gooijer ₁ , Karen Harkema ₁ , Marieke Hazewinkel ₁ , Susan Snijder ₁ , Kees Pouwer ₁

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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 sp³-character, hence being very interesting 3D scaffolds. The compounds synthesized were added to the compound collection of the European Lead Factory.

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