Bioconjugation chemistry has emerged as a powerful tool for the modification of diverse
biomolecules under mild conditions. Tetrazole, initially proposed as a bioorthogonal …

Triazoles are privileged structural motifs that are embedded in a number of molecules with
interesting biological activities. In this work, we developed a practical and general synthetic …

ABSTRACT Introduction The effectiveness of Fragment-based drug design (FBDD) for
targeting challenging therapeutic targets has been hindered by two factors: the small library …

Thiohydantoin represents a significant class of biologically active privileged heterocyclic
scaffolds. Herein, we present a convenient and robust DNA-compatible method for …

While DNA-encoded macrocyclic libraries have gained substantial attention and several hit
compounds have been identified from DNA-encoded library technology, efficient on-DNA …

DNA-encoded library (DEL) technology holds exciting potential for discovering novel
therapeutic macrocyclic peptides (MPs). Herein, we describe the development of a DEL …

Thiazolidione, conferring drug-like properties, is an important heterocycle that widely exists
in medicinally relevant molecules. In this work, by efficiently assembling various DNA …

Utilizing already existing DNA-encoded libraries (DELs) for the generation of a distinct DEL
represents an expedited strategy for expanding the chemical space. Herein, we leverage the …

The incorporation of N-containing heterocycles with potential bioactivity into DNA-encoded
chemical libraries (DELs) represents an important approach to synthesizing medicinally …

Construction of DNA-encoded chemical libraries that contain focused pharmacophores is of
great value for high-throughput hit discovery. Enaminone serves as a privileged scaffold in a …