In 2013, the first review article recommending the introduction of the sulfoximine group as a versatile pharmacophore to the medicinal chemist’s toolbox was published.[1] Sulfoximines, the mono-aza analoges of sulfones, by then had received little interest in drug discovery, despite their very interesting properties.[1,2] However, interest in this unusual functional group has increased substantially in recent years, which is exemplified by the selection of several novel sulfoximine compounds for clinical evaluation (e.g. atuveciclib, BAY 1251152, AZD6738). Moreover, a significant and ever-increasing number of sulfoximines featured in scientific articles and life science patent applications, as well as commercially available sulfoximine building blocks, serve to highlight the increased acceptance of this functional group by the drug discovery community. This presentation provides an overview on the use of the formerly neglected sulfoximine group in drug discovery since 2013, focusing on selected use cases from the literature.

Sulfoximines in drug discovery revisited: What has happened since 2013?

2019 Fall National Meeting

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