Identification of 1H-pyrazolo[3,4-b]pyridine derivatives as potent ALK-L1196M inhibitors

Identification of 1H-pyrazolo[3,4-b]pyridine derivatives as potent ALK-L1196M inhibitors

Anaplastic lymphoma kinase (ALK) has been recognised as a promising molecular target of targeted therapy for NSCLC. We performed SAR study of pyrazolo[3,4-b]pyridines to override crizotinib resistance caused by ALK-L1196M mutation and identified a novel and potent L1196M inhibitor, 10g. 10g displaye...

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Veröffentlicht in:Journal of enzyme inhibition and medicinal chemistry 2019-01, Vol.34 (1), p.1426-1438
Hauptverfasser: Nam, Yunju, Hwang, Dongkeun, Kim, Namdoo, Seo, Hong-Seog, Selim, Khalid B., Sim, Taebo
Format: Artikel
Sprache:eng
Schlagworte:
ALK-L1196M mutant
Anaplastic lymphoma kinase
pyrazolopyridine-based inhibitor
Research Paper
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Zusammenfassung:Anaplastic lymphoma kinase (ALK) has been recognised as a promising molecular target of targeted therapy for NSCLC. We performed SAR study of pyrazolo[3,4-b]pyridines to override crizotinib resistance caused by ALK-L1196M mutation and identified a novel and potent L1196M inhibitor, 10g. 10g displayed exceptional enzymatic activities (
ISSN:1475-6366
1475-6374
DOI:10.1080/14756366.2019.1639694