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Table 1 Reported IDO inhibitors

From: Targeting the indoleamine 2,3-dioxygenase pathway in cancer

Agent Mechanism First author, year
D-1MT Tryptophan mimetic; D isoform of MT; Transcriptional suppressor of IDO Metz 2012 [32]
L-1MT Tryptophan mimetic; L isoform of MT; selective IDO1 inhibitor Opitz 201 [39]
MTH-Trp Tryptophan mimetic; transcriptional suppressor of IDO Okamoto 2007 [92]
β-carbolines Tryptophan mimetic; IDO and TDO inhibitor Eguchi 1984 [93]
Naphthoquinone-based Pharmacophore of natural product annulin B; indole mimetic; IDO inhibitor Kumar 2008 [94]
S-allyl-brassinin Phytoalexin; indole mimetic Gaspari 2006 [95]
S-benzyl-brassinin Phytoalexin; indole mimetic Gaspari 2006 [95]
5-Bromo-brassinin Phytoalexin; indole mimetic Banerjee 2008 [96]
Phenylimidazole-based Computationally designed synthetic IDO inhibitor Kumar 2008 [94]
4-phenylimidazole Heme ligand in IDO enzyme Sono 1989 [97]
Exiguamine A Non-tryptophan analogue Harry 2006 [98]
NSC401366 Non-indolic IDO inhibitor Vottero 2006 [99]
  1. IDO Indoleamine-2,3-dioxygenase 1, 1MT 1-methyl-DL-tryptophan, MTH-Trp methylthiohydantoin-dl-tryptophan, TDO tryptophan-2,3-dioxygenase