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Structure-Guided Evolution of Potent and Selective CHK1 Inhibitors through Scaffold Morphing

[Image: see text] Pyrazolopyridine inhibitors with low micromolar potency for CHK1 and good selectivity against CHK2 were previously identified by fragment-based screening. The optimization of the pyrazolopyridines to a series of potent and CHK1-selective isoquinolines demonstrates how fragment-grow...

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Detalhes bibliográficos
Main Authors: Reader, John C., Matthews, Thomas P., Klair, Suki, Cheung, Kwai-Ming J., Scanlon, Jane, Proisy, Nicolas, Addison, Glynn, Ellard, John, Piton, Nelly, Taylor, Suzanne, Cherry, Michael, Fisher, Martin, Boxall, Kathy, Burns, Samantha, Walton, Michael I., Westwood, Isaac M., Hayes, Angela, Eve, Paul, Valenti, Melanie, de Haven Brandon, Alexis, Box, Gary, van Montfort, Rob L. M., Williams, David H., Aherne, G. Wynne, Raynaud, Florence I., Eccles, Suzanne A., Garrett, Michelle D., Collins, Ian
Formato: Artigo
Idioma:Inglês
Publicado em: American Chemical Society 2011
Acesso em linha:https://ncbi.nlm.nih.gov/pmc/articles/PMC3241339/
https://ncbi.nlm.nih.gov/pubmed/22111927
https://ncbi.nlm.nih.govhttp://dx.doi.org/10.1021/jm2007326
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