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- W3171839490 abstract "A series of exiguamine A analogues were designed and synthesized via 15 steps. Their inhibitory activities against IDO1 were tested and the structure-activity relationships were studied. Most compounds exhibited potent IDO1 inhibitory activities with IC50 values at the level of 10−7–10−8 M. Compound 21f was the most potent IDO1 inhibitor with an IC50 value of 65.3 nM, which was comparable with the positive control drug epacadostat (IC50 = 46 nM). Moreover, compound 21f showed higher selectivity for IDO1 over tryptophan 2,3-dioxygenase (TDO) and no cytotoxicity at its effective concentration, rending it justifiable for further optimization and evaluation." @default.
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- W3171839490 date "2021-11-01" @default.
- W3171839490 modified "2023-09-27" @default.
- W3171839490 title "Design, synthesis and biological evaluation of exiguamine A analogues as IDO1 inhibitors" @default.
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- W3171839490 doi "https://doi.org/10.1016/j.ejmech.2021.113631" @default.
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