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合成一类新型选择性TNIK抑制剂并评估其抗结直肠癌作用,PK研究通过美迪西进行

2023-07-05
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The Traf2- and Nck-interacting protein kinase (TNIK) is a downstream signal protein of the Wnt/β-catenin pathway and has been thought of as a potential target for the treatment of colorectal cancer. SAR analysis leads to the identification of a number of potent TNIK inhibitors with Compound 21k being the most active one. Preliminary assessment for the pharmacokinetic properties of Compound 21k was carried out through services provided by Medicilon.

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Reference:

Yueshan Li, et al. Discovery of 3,4-Dihydrobenzo[ f][1,4]oxazepin-5(2 H)-one Derivatives as a New Class of Selective TNIK Inhibitors and Evaluation of Their Anti-Colorectal Cancer Effects. J Med Chem. 2022 Feb 10;65(3):1786-1807.  doi: 10.1021/acs.jmedchem.1c00672.  

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