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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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
פורמט: Artigo
שפה:Inglês
יצא לאור: American Chemical Society 2011
גישה מקוונת: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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