Highlights•High-throughput docking of small molecules is very successful in hit identification,
particularly for screening mainly rigid fragments.•Classical force fields with implicit solvent …

Small-molecule inhibitors of indoleamine 2, 3-dioxygenase-1 (IDO1) are emerging at the
vanguard of experimental agents in oncology. Here, pioneers of this new drug class provide …

The tryptophan catabolic enzyme indoleamine 2, 3-dioxygenase-1 (IDO1) has attracted
enormous attention in driving cancer immunosuppression, neovascularization, and …

Various pathologies of the central nervous system (CNS) are accompanied by alterations in
tryptophan metabolism. The main metabolic route of tryptophan degradation is the …

IDO1 (indoleamine 2, 3-dioxygenase 1) is a member of a unique class of mammalian haem
dioxygenases that catalyse the oxidative catabolism of the least-abundant essential amino …

Since the discovery of indoleamine 2, 3-dioxygenase 1 (IDO1) as an attractive target for
anticancer therapy in 2003, the search for inhibitors has been intensely pursued both in …

A p-TsOH-mediated 1, 3-dipolar cycloaddition of nitroolefins and sodium azide for the
synthesis of 4-aryl-NH-1, 2, 3-triazoles has been developed. p-TsOH was discovered as a …

Cu (II)-promoted ortho alkynylation of arenes and heteroarenes with terminal alkynes has
been developed to prepare aryl alkynes. A variety of arenes and terminal alkynes bearing …

Highlights•Advances in the combination of the CuAAC reaction with direct screening.•Before
library assembly, the bioisosteric potential of 1, 2, 3-triazole should be confirmed.•The …

Indoleamine 2, 3-dioxygenase 1 (IDO1), promoting immune escape of tumors, is a
therapeutic target for the cancer immunotherapy. A number of IDO1 inhibitors have been …