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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Huvudupphovsmän: 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
Materialtyp: Artigo
Språk:Inglês
Publicerad: American Chemical Society 2011
Länkar: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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