Spirocyclic scaffolds are incorporated in various approved drugs and drug candidates. The
increasing interest in less planar bioactive compounds has given rise to the development of …

Targeted covalent inhibitors (TCIs) are designed to bind poorly conserved amino acids by
means of reactive groups, the so-called warheads. Currently, targeting noncatalytic cysteine …

Activity-based protein profiling (ABPP) is a technique that uses highly selective active-site
targeted chemical probes to label and monitor the state of proteins. ABPP integrates the …

Mutations in many members of the set of human lysosomal glycoside hydrolases cause a
wide range of lysosomal storage diseases. As a result, much effort has been directed toward …

The development of small molecule activity-based probes (ABPs) is an evolving and
powerful area of chemistry. There is a major need for synthetically accessible and specific …

A smart theranostic prodrug IMC-FDU-TZBC-NO2, releasing active drug on-demand based
on hypoxia-activated and indomethacin-mediated, for solid tumor imaging and efficient …

This work reports an efficient diastereoselective synthetic methodology for the preparation of
phosphorus substituted cyanoaziridines through the nucleophilic addition of TMSCN, as …

DT-diaphorase, which catalyzes the reduction of various biological substances like
quinones, is overexpressed in some malignant tumors. However, exploiting this attractive …

A divergent synthesis to eight d‐xylo‐and l‐arabino‐cyclophellitol and cyclophellitol
aziridine derivatives is described. The syntheses start from d‐xylose and feature asymmetric …

We report an approach to the diastereoselective synthesis of 1, 2‐disubstituted heterocyclic
aziridines. A Brønsted acid‐catalyzed conjugate addition of anilines to trisubstituted …