Development of ‘DFG-out’ inhibitors of gatekeeper mutant kinases

HG-7-85-01(22) and HG-7-86-01(26) are thiazolo[5,4-b]pyridine containing type II tyrosine kinase inhibitors with potent cellular activity against both wild-type and ‘gatekeeper’ mutant T315I- Bcr-Abl. Here we report on the ‘hybrid design’ concept and subsequent structure activity guided optimization...

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Detalhes bibliográficos
Main Authors: Choi, Hwan Geun, Zhang, Jianming, Weisberg, Ellen, Griffin, James D., Sim, Taebo, Gray, Nathanael S.
Formato: Artigo
Idioma:Inglês
Publicado em: 2012
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Article
Acesso em linha:https://ncbi.nlm.nih.gov/pmc/articles/PMC3415686/
https://ncbi.nlm.nih.gov/pubmed/22819762
https://ncbi.nlm.nih.govhttp://dx.doi.org/10.1016/j.bmcl.2012.06.036
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