Discovery of pyrazolopyrimidine derivatives as novel inhibitors of ataxia telangiectasia and rad3 related protein (ATR)

[Display omitted] The ATR pathway is a critical mediator of the replication stress response in cells. In aberrantly proliferating cancer cells, this pathway can help maintain sufficient genomic integrity for cancer cell progression. Herein we describe the discovery of 19, a pyrazolopyrimidine-contai...

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Veröffentlicht in:	Bioorganic & medicinal chemistry letters 2017-02, Vol.27 (4), p.750-754
Hauptverfasser:	Ramachandran, Sreekanth A., Jadhavar, Pradeep S., Singh, Manvendra P., Sharma, Ankesh, Bagle, Gaurav N., Quinn, Kevin P., Wong, Po-yin, Protter, Andrew A., Rai, Roopa, Pham, Son M., Lindquist, Jeffrey N.
Format:	Artikel
Sprache:	eng
Schlagworte:	Ataxia Telangiectasia Mutated Proteins - antagonists & inhibitors Ataxia Telangiectasia Mutated Proteins - metabolism ATR DNA damage Drug Evaluation, Preclinical HTS Humans Inhibitory Concentration 50 Phosphatidylinositol 3-Kinases - chemistry Phosphatidylinositol 3-Kinases - metabolism PI3K Protein Binding Protein Kinase Inhibitors - chemistry Protein Kinase Inhibitors - metabolism Protein-Serine-Threonine Kinases - antagonists & inhibitors Protein-Serine-Threonine Kinases - metabolism Pyrazoles - chemistry Pyrazoles - metabolism Pyrazolopyrimidine Pyridines - chemistry Pyridines - metabolism Pyrimidines - chemistry Pyrimidines - metabolism
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Zusammenfassung:	[Display omitted] The ATR pathway is a critical mediator of the replication stress response in cells. In aberrantly proliferating cancer cells, this pathway can help maintain sufficient genomic integrity for cancer cell progression. Herein we describe the discovery of 19, a pyrazolopyrimidine-containing inhibitor of ATR via a strategic repurposing of compounds targeting PI3K.
ISSN:	0960-894X 1464-3405
DOI:	10.1016/j.bmcl.2017.01.045