Discovery of Pyrazolo[1,5-a]pyrimidine TTK Inhibitors: CFI-402257 is a Potent, Selective, Bioavailable Anticancer Agent

[Image: see text] This work describes a scaffold hopping exercise that begins with known imidazo[1,2-a]pyrazines, briefly explores pyrazolo[1,5-a][1,3,5]triazines, and ultimately yields pyrazolo[1,5-a]pyrimidines as a novel class of potent TTK inhibitors. An X-ray structure of a representative compo...

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Udgivet i:ACS Med Chem Lett
Main Authors: Liu, Yong, Laufer, Radoslaw, Patel, Narendra Kumar, Ng, Grace, Sampson, Peter B., Li, Sze-Wan, Lang, Yunhui, Feher, Miklos, Brokx, Richard, Beletskaya, Irina, Hodgson, Richard, Plotnikova, Olga, Awrey, Donald E., Qiu, Wei, Chirgadze, Nickolay Y., Mason, Jacqueline M., Wei, Xin, Lin, Dan Chi-Chia, Che, Yi, Kiarash, Reza, Fletcher, Graham C., Mak, Tak W., Bray, Mark R., Pauls, Henry W.
Format: Artigo
Sprog:Inglês
Udgivet: American Chemical Society 2016
Online adgang:https://ncbi.nlm.nih.gov/pmc/articles/PMC4948001/
https://ncbi.nlm.nih.gov/pubmed/27437075
https://ncbi.nlm.nih.govhttp://dx.doi.org/10.1021/acsmedchemlett.5b00485
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