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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Detalles Bibliográficos
Autores principales: 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: Online Artículo Texto
Lenguaje:English
Publicado: American Chemical Society 2011
Acceso en línea:https://www.ncbi.nlm.nih.gov/pmc/articles/PMC3241339/
https://www.ncbi.nlm.nih.gov/pubmed/22111927
http://dx.doi.org/10.1021/jm2007326

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