Introduction of a Methyl Group Curbs Metabolism of Pyrido[3,4-d]pyrimidine Monopolar Spindle 1 (MPS1) Inhibitors and Enables the Discovery of the Phase 1 Clinical Candidate N(2)-(2-Ethoxy-4-(4-methyl-4H-1,2,4-triazol-3-yl)phenyl)-6-methyl-N(8)-neopentylpyrido[3,4-d]pyrimidine-2,8-diamine (BOS172722)

[Image: see text] Monopolar spindle 1 (MPS1) occupies a central role in mitosis and is one of the main components of the spindle assembly checkpoint. The MPS1 kinase is an attractive cancer target, and herein, we report the discovery of the clinical candidate BOS172722. The starting point for our wo...

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Detalles Bibliográficos
Autores principales: Woodward, Hannah L., Innocenti, Paolo, Cheung, Kwai-Ming J., Hayes, Angela, Roberts, Jennie, Henley, Alan T., Faisal, Amir, Mak, Grace Wing-Yan, Box, Gary, Westwood, Isaac M., Cronin, Nora, Carter, Michael, Valenti, Melanie, De Haven Brandon, Alexis, O’Fee, Lisa, Saville, Harry, Schmitt, Jessica, Burke, Rosemary, Broccatelli, Fabio, van Montfort, Rob L. M., Raynaud, Florence I., Eccles, Suzanne A., Linardopoulos, Spiros, Blagg, Julian, Hoelder, Swen
Formato: Online Artículo Texto
Lenguaje:English
Publicado: American Chemical Society 2018
Acceso en línea:https://www.ncbi.nlm.nih.gov/pmc/articles/PMC6166229/
https://www.ncbi.nlm.nih.gov/pubmed/30199249
http://dx.doi.org/10.1021/acs.jmedchem.8b00690

Internet

https://www.ncbi.nlm.nih.gov/pmc/articles/PMC6166229/
https://www.ncbi.nlm.nih.gov/pubmed/30199249
http://dx.doi.org/10.1021/acs.jmedchem.8b00690

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