Given the ubiquity of heterocycles in biologically active molecules, transformations with the
capacity to modify such molecular skeletons with modularity remain highly desirable. Ring …

Hydrogen bonds (HB) s are the most abundant motifs in biological systems. They play a key
role in determining protein–ligand binding affinity and selectivity. We designed two …

In recent years, tumor immunotherapy, aimed at increasing the activity of immune cells and
reducing immunosuppressive effects, has attracted wide attention. Among them, immune …

Considering the importance of heterocycles, significantly represented in medicinal chemistry
and drug development, the single-atom insertion technique and transmutation strategy …

Since the discovery of the implication of indoleamine 2, 3-dioxygenase 1 (IDO1) in tumoral
immune resistance in 2003, the search for inhibitors has been intensely pursued both in …

Indoleamine 2, 3-dioxygenase 1 (IDO1), a heme-containing enzyme that mediates the rate-
limiting step in the metabolism of l-tryptophan to kynurenine, has been widely explored as a …

Hematopoietic progenitor kinase 1 (HPK1) serves a key immunosuppressive role as a
negative regulator of T-cell receptor (TCR) signaling. HPK1 loss-of-function is associated …

3, 3-Disubstituted oxetanes have been utilized as bioisosteres for gem-dimethyl and
cyclobutane functionalities. We report the discovery of a novel class of oxetane indole-amine …

The science of drug discovery involves multiparameter optimization of molecular structures
through iterative design–make–test cycles. For medicinal chemistry library synthesis …

Modern organic chemistry is a titan supporting and reinforcing pharmaceutical, agricultural,
food and material science products. Over the past decades, the organic compounds market …