The vinyl sulfone motif as a structural unit for novel drug design and discovery

IntroductionVinyl sulfones are a special sulfur-containing structural unit that have attracted considerable attention, owing to their important role in serving as key structural motifs of various biologically active compounds as well as serving as versatile building blocks for organic transformations. The synthetic strategy of vinyl sulfone derivatives has been substantially upgraded over the past 30 years, and the wide application of this functional group in drug design and discovery has been promoted.Area CoveredIn this review, the authors review the application of vinyl sulfones in drug discovery and select optimized compounds which might have significant impact or potential inspiration for drug design.Expert opinionVinyl sulfones have been reported to target various macromolecular targets via non-covalent or covalent interactions, including multiple kinases, tubulin, cysteine protease, transcription factor, and so on. Thus, it has been significantly applied as a privileged scaffold in the design of anticancer, anti-infective, anti-inflammatory, and neuroprotective agents. However, much work remains to be done to improve the drug-like properties, such as chemical and metabolic stability, ADME, and toxicity. Besides, the chemical space of vinyl sulfones needs to be expanded, including but not limited to the design of constrained endocyclic and exocyclic vinyl sulfones.

Automated summary

Vinyl sulfones play important roles in drug discovery as structural motifs and versatile building blocks. They target various macromolecular targets and have been applied in the design of anticancer, anti-infective, anti-inflammatory, and neuroprotective agents. However, further improvement is needed in terms of drug-like properties and the chemical space of vinyl sulfones.