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Indoleamine 2,3-dioxygenase (IDO) is a heme dioxygenase which has been shown to be involved in the pathological immune escape of diseases such as cancer. The synthesis and structure-activity relationships (SAR) of a novel series of IDO inhibitors based on the indol-2-yl ethanone scaffold is described. In vitro and in vivo biological activities have been evaluated, leading to compounds with IC(50) values in the micromolar range in both tests. Introduction of small substituents in the 5- and 6-positions of the indole ring, indole N-methylation and variations of the aromatic side chain are all well tolerated. An iron coordinating group on the linker is a prerequisite for biological activity, thus corroborating the virtual screening results.

Original publication

DOI

10.1016/j.bmc.2010.12.032

Type

Journal article

Journal

Bioorg Med Chem

Publication Date

15/02/2011

Volume

19

Pages

1550 - 1561

Keywords

Catalytic Domain, Cell Line, Ethane, Humans, Indoleamine-Pyrrole 2,3,-Dioxygenase, Indoles, Models, Molecular, Protein Interaction Domains and Motifs, Structure-Activity Relationship