Back to Search
Start Over
Discovery of pyrazolopyrimidine derivatives as novel inhibitors of ataxia telangiectasia and rad3 related protein (ATR).
- Source :
-
Bioorganic & medicinal chemistry letters [Bioorg Med Chem Lett] 2017 Feb 15; Vol. 27 (4), pp. 750-754. Date of Electronic Publication: 2017 Jan 16. - Publication Year :
- 2017
-
Abstract
- 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.<br /> (Copyright © 2017 Elsevier Ltd. All rights reserved.)
- Subjects :
- Ataxia Telangiectasia Mutated Proteins metabolism
Drug Evaluation, Preclinical
Humans
Inhibitory Concentration 50
Phosphatidylinositol 3-Kinases chemistry
Phosphatidylinositol 3-Kinases metabolism
Protein Binding
Protein Kinase Inhibitors metabolism
Protein Serine-Threonine Kinases antagonists & inhibitors
Protein Serine-Threonine Kinases metabolism
Pyrazoles metabolism
Pyridines metabolism
Pyrimidines metabolism
Ataxia Telangiectasia Mutated Proteins antagonists & inhibitors
Protein Kinase Inhibitors chemistry
Pyrazoles chemistry
Pyridines chemistry
Pyrimidines chemistry
Subjects
Details
- Language :
- English
- ISSN :
- 1464-3405
- Volume :
- 27
- Issue :
- 4
- Database :
- MEDLINE
- Journal :
- Bioorganic & medicinal chemistry letters
- Publication Type :
- Academic Journal
- Accession number :
- 28131712
- Full Text :
- https://doi.org/10.1016/j.bmcl.2017.01.045