Discovery of 3, 6-diaryl-1H-pyrazolo[3, 4-b]pyridines as potent anaplastic lymphoma kinase (ALK) inhibitors. Issue 7 (1st April 2019)

• Record Type: Journal Article
• Authors: Chen, Changwei; Pan, Peichen; Deng, Ziyang; Wang, Dahai; Wu, Qifan; Xu, Lei; Hou, Tingjun; Cui, Sunliang
• Is Part Of: Bioorganic & medicinal chemistry letters. Volume 29:Issue 7(2019)
• Page Start: 912
• Page End: 916
• Publication Date: 2019-04-01
• Subjects: ALK -- Kinase -- Inhibitor -- Anti-tumor -- 1H-pyrazolo[3, 4, -b]pyridine; Bioorganic chemistry -- Periodicals; Pharmaceutical chemistry -- Periodicals; 572
• DOI: 10.1016/j.bmcl.2019.01.037
• Languages: English
• ISSNs: 0960-894X

Abstract

Graphical abstract: Abstract: A new series of 3, 6-diaryl-1 H -pyrazolo[3, 4- b ]pyridine compounds have been discovered as potent anaplastic lymphoma kinase (ALK) inhibitors. The 4-hydroxyphenyl in the 6-position of 1 H -pyrazolo[3, 4- b ]pyridine were crucial and a fluorine atom substitution could give promising inhibitory activity. The IC50 of compound9v against ALK was up to 1.58 nM and a binding mechanism was proposed.