Vinyl sulfones and sulfonamides are valued for their use as electrophilic warheads in
covalent protein inhibitors. Conversely, the S (VI) aza-isosteres thereof, vinyl sulfoximines …

Protein arylation has attracted much attention for developing new classes of bioconjugates
with improved properties. Here, we have evaluated 2-sulfonylpyrimidines as covalent …

Reported here is the synthesis of a class of semi‐oxamide vinylogous thioesters, designated
STEFs, and the use of these agents as new electrophilic warheads. This work includes …

Traditional biochemical target-based and phenotypic cell-based screening approaches to
drug discovery have produced the current covalent and non-covalent pharmacopoeia …

Flipping the polarity switch | Nature Chemical Biology Skip to main content Thank you for
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Sulfonamides are one of the most important pharmacophores in medicinal chemistry, and
sulfonamide analogues have gained substantial interest in recent years. However, the …

Drug candidates are generally discovered using biochemical screens employing an isolated
target protein or by utilizing cell-based phenotypic assays. Both noncovalent and covalent …

The occurrence of sulfoximines and sulfonimidoyl groups in biologically active molecules
within pharmaceuticals and agrochemicals has notably increased in the past decade. This …

The discovery of innovative small-molecule drugs is a challenging endeavor. Medicinal
chemists need to continuously optimize the properties of bioactive compounds while at the …

Drug candidates that form covalent linkages with their target proteins have been
underexplored compared with the conventional counterparts that modulate biological …