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• W2968669259 abstract "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 (<0.5 nM of IC50) against ALK-L1196M as well as against ALK-wt. In addition, 10g is an extremely potent inhibitor of ROS1 (<0.5 nM of IC50) and displays excellent selectivity over c-Met. Moreover, 10g strongly suppresses proliferation of ALK-L1196M-Ba/F3 and H2228 cells harbouring EML4-ALK via apoptosis and the ALK signalling blockade. The results of molecular docking studies reveal that, in contrast to crizotinib, 10g engages in a favourable interaction with M1196 in the kinase domain of ALK-L1196M and hydrogen bonding with K1150 and E1210. This SAR study has provided a useful insight into the design of novel and potent inhibitors against ALK gatekeeper mutant." @default.
• W2968669259 created "2019-08-22" @default.
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• W2968669259 date "2019-01-01" @default.
• W2968669259 modified "2023-10-16" @default.
• W2968669259 title "Identification of 1<i>H</i>-pyrazolo[3,4-b]pyridine derivatives as potent ALK-L1196M inhibitors" @default.
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• W2968669259 doi "https://doi.org/10.1080/14756366.2019.1639694" @default.
• W2968669259 hasPubMedCentralId "https://www.ncbi.nlm.nih.gov/pmc/articles/6713165" @default.
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