1,2,3-Triazoles as inhibitors of indoleamine 2,3-dioxygenase 2 (IDO2)

Ute F. Röhrig,Somi Reddy Majjigapu, Daniela Caldelari,Nahzli Dilek, Patrick Reichenbach,Kelly Ascencao,Melita Irving,George Coukos,Pierre Vogel,Vincent Zoete,Olivier Michielin

Bioorganic & Medicinal Chemistry Letters（2016）

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摘要

•IDO2 is a potential target in cancer immunotherapy.•4-Aryl-1,2,3-triazoles were synthesized and tested in cellular assays for mIDO2 inhibition.•Best compound has an IC50 value of 51μM for mIDO2, twofold selectivity over hIDO1, and is not cytotoxic.

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关键词

Indoleamine 2,3-dioxygenase,Cancer immunotherapy,Molecular modeling,Cellular assays,Tryptophan metabolism

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