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Indoleamine 2,3-dioxygenase (IDO) is an important new therapeutic target for the treatment of cancer. With the aim of discovering novel IDO inhibitors, a virtual screen was undertaken and led to the discovery of the keto-indole derivative 1a endowed with an inhibitory potency in the micromolar range. Detailed kinetics were performed and revealed an uncompetitive inhibition profile. Preliminary SARs were drawn in this series and corroborated the putative binding orientation as suggested by docking.

Original publication

DOI

10.1016/j.ejmech.2011.02.049

Type

Journal article

Journal

Eur J Med Chem

Publication Date

07/2011

Volume

46

Pages

3058 - 3065

Keywords

Animals, Antineoplastic Agents, Cell Line, Tumor, Databases, Chemical, Drug Discovery, Enzyme Assays, Enzyme Inhibitors, Escherichia coli, Gene Expression, High-Throughput Screening Assays, Humans, Indoleamine-Pyrrole 2,3,-Dioxygenase, Indoles, Mice, Molecular Docking Simulation, Neoplasm Proteins, Recombinant Proteins, Structure-Activity Relationship, Tryptophan