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• W2531384845 abstract "Uncontrolled metabolism of l-tryptophan (l-Trp) in the immune system has been recognized as a critical cellular process in immune tolerance. Indoleamine 2,3-dioxygenase 1 (IDO1) enzyme plays an important role in the metabolism of a local l-Trp through the kynurenine pathway in the immune systems. In this regard, IDO1 has emerged as a therapeutic target for the treatment of diseases that are associated with immune suppression like chronic infections, cancer, and others. In this study, we synthesized a series of pyridopyrimidine, pyrazolopyranopyrimidine, and dipyrazolopyran derivatives. Further lead optimizations directed to the identification of potent compounds, 4j and 4l (IC50 = 260 and 151 nM, respectively). These compounds also exhibited IDO1 inhibitory activities in the low nanomolar range in MDA-MB-231 cells with very low cytotoxicity. Stronger selectivity for the IDO1 enzyme (>300-fold) over tryptophan 2,3-dioxygenase (TDO) enzyme was also observed for these compounds. Hence, these fused heterocyclic compounds are attractive candidates for the advanced study of IDO1-dependent cellular function and immunotherapeutic applications." @default.
• W2531384845 created "2016-10-21" @default.
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• W2531384845 date "2016-10-20" @default.
• W2531384845 modified "2023-10-18" @default.
• W2531384845 title "Fused Heterocyclic Compounds as Potent Indoleamine-2,3-dioxygenase 1 Inhibitors" @default.
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• W2531384845 doi "https://doi.org/10.1021/acsmedchemlett.6b00359" @default.
• W2531384845 hasPubMedCentralId "https://www.ncbi.nlm.nih.gov/pmc/articles/5150662" @default.
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