新型吲哚胺2,3-双加氧酶抑制剂系列的鉴定与优化
Identification and optimization of a novel series of indoleamine 2,3-dioxygenase inhibitors.
作者信息
Markwalder Jay A, Seitz Steven P, Blat Yuval, Elkin Lisa, Hunt John T, Pabalan Jonathan G, Jure-Kunkel Maria N, Vite Gregory D, Covello Kelly
机构信息
Oncology Chemistry, Bristol-Myers Squibb Research and Development, Princeton, NJ 08543-5400, United States.
Oncology Chemistry, Bristol-Myers Squibb Research and Development, Princeton, NJ 08543-5400, United States.
出版信息
Bioorg Med Chem Lett. 2017 Feb 1;27(3):582-585. doi: 10.1016/j.bmcl.2016.12.015. Epub 2016 Dec 7.
The discovery of a series of structurally-novel biaryl urea IDO inhibitors is described. Optimization of a micromolar hit through iterative cycles of synthesis and screening in an assay measuring IDO-mediated intracellular conversion of tryptophan to kynurenine led to potent inhibitors with favorable selectivity and metabolic stability profiles.
本文描述了一系列结构新颖的联芳基脲吲哚胺2,3-双加氧酶（IDO）抑制剂的发现。通过在测量IDO介导的色氨酸向犬尿氨酸细胞内转化的试验中进行合成和筛选的迭代循环，对微摩尔活性的起始化合物进行优化，得到了具有良好选择性和代谢稳定性的强效抑制剂。
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