Discovery of 3,6-diaryl-1H-pyrazolo[3,4-b]pyridines as potent anaplastic lymphoma kinase (ALK) inhibitors |
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| Authors: | Changwei Chen Peichen Pan Ziyang Deng Dahai Wang Qifan Wu Lei Xu Tingjun Hou Sunliang Cui |
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| Institution: | 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 |
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| Abstract: | A new series of 3,6-diaryl-1H-pyrazolo3,4-b]pyridine compounds have been discovered as potent anaplastic lymphoma kinase (ALK) inhibitors. The 4-hydroxyphenyl in the 6-position of 1H-pyrazolo3,4-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. |
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| Keywords: | ALK Kinase Inhibitor Anti-tumor Corresponding authors |
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