Discovery of 3,6-diaryl-1H-pyrazolo[3,4-b]pyridines as potent anaplastic lymphoma kinase (ALK) inhibitors

Bioorg Med Chem Lett. 2019 Apr 1;29(7):912-916. doi: 10.1016/j.bmcl.2019.01.037.

Changwei Chen ¹, Peichen Pan ¹, Ziyang Deng ¹, Dahai Wang ¹, Qifan Wu ¹, Lei Xu ², Tingjun Hou ³, Sunliang Cui ⁴

Affiliations

1 College of Pharmaceutical Sciences, Zhejiang University, 866 Yuhangtang Road, Hangzhou 310058, PR China.
2 Institute of Bioinformatics and Medical Engineering, School of Electrical and Information Engineering, Jiangsu University of Technology, Changzhou 213001, PR China.
3 College of Pharmaceutical Sciences, Zhejiang University, 866 Yuhangtang Road, Hangzhou 310058, PR China. Electronic address: tingjunhou@zju.edu.cn.
4 College of Pharmaceutical Sciences, Zhejiang University, 866 Yuhangtang Road, Hangzhou 310058, PR China. Electronic address: slcui@zju.edu.cn.

PMID: 30777610 DOI: 10.1016/j.bmcl.2019.01.037

Abstract

A new series of 3,6-diaryl-1H-pyrazolo[3,4-b]pyridine compounds have been discovered as potent anaplastic lymphoma kinase (ALK) inhibitors. The 4-hydroxyphenyl in the 6-position of 1H-pyrazolo[3,4-b]pyridine were crucial and a fluorine atom substitution could give promising inhibitory activity. The IC₅₀ of compound 9v against ALK was up to 1.58 nM and a binding mechanism was proposed.

Keywords

1H-pyrazolo[3,4,-b]pyridine; ALK; Anti-tumor; Inhibitor; Kinase.

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