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Science Translational Medicine, ISSN 1946-6234, 11/2017, Volume 9, Issue 414
Journal Article
Cancer Discovery, ISSN 2159-8274, 04/2015, Volume 5, Issue 4, pp. 424 - 437
Journal Article
Molecular Cancer Therapeutics, ISSN 1535-7163, 08/2010, Volume 9, Issue 8, pp. 2344 - 2353
Journal Article
Journal Article
Molecular Cancer Therapeutics, ISSN 1535-7163, 04/2011, Volume 10, Issue 4, pp. 591 - 602
Checkpoint kinase 1 (CHK1) is an essential serine/threonine kinase that responds to DNA damage and stalled DNA replication. CHK1 is essential for maintenance... 
CANCER-CELLS | PHASE | ACTIVATION | DNA-DAMAGE CHECKPOINT | PRECLINICAL PHARMACOLOGY | ONCOLOGY | PHOSPHORYLATION | ABROGATION | CYCLIN-DEPENDENT KINASE | DISCOVERY | ATR | Protein Kinases - metabolism | Protein Kinases - genetics | Cyclin-Dependent Kinases - metabolism | Apoptosis - drug effects | DNA Replication - drug effects | Humans | Pyridinium Compounds - administration & dosage | Deoxycytidine - pharmacology | Immunoblotting | Pyrimidines - chemistry | Antimetabolites, Antineoplastic - administration & dosage | Protein Kinase Inhibitors - chemistry | Pyrazoles - chemistry | DNA Breaks, Double-Stranded - drug effects | RNA Interference | Antimetabolites, Antineoplastic - pharmacology | Molecular Structure | Cyclin-Dependent Kinases - genetics | Protein-Serine-Threonine Kinases - metabolism | Pyrazoles - pharmacology | Drug Screening Assays, Antitumor - methods | Pyrimidines - administration & dosage | Protein-Serine-Threonine Kinases - genetics | Bridged Bicyclo Compounds, Heterocyclic - administration & dosage | Pyrimidines - pharmacology | Xenograft Model Antitumor Assays | Protein Kinase Inhibitors - administration & dosage | Pyridinium Compounds - pharmacology | Bridged Bicyclo Compounds, Heterocyclic - pharmacology | Pyrazoles - administration & dosage | Animals | Tumor Burden - drug effects | Antineoplastic Combined Chemotherapy Protocols - therapeutic use | Mice, Nude | Cell Line, Tumor | Checkpoint Kinase 2 | Checkpoint Kinase 1 | Mice | Protein Kinase Inhibitors - pharmacology | Histones - metabolism | Deoxycytidine - analogs & derivatives
Journal Article
Journal Article
Cancer Discovery, ISSN 2159-8274, 07/2018, Volume 8, Issue 7, pp. 836 - 849
The receptor tyrosine kinase rearranged during transfection (RET) is an oncogenic driver activated in multiple cancers, including non-small cell lung cancer... 
CELL LUNG-CANCER | TYROSINE KINASE INHIBITORS | CABOZANTINIB | ONCOLOGY | ADENOCARCINOMA | CRIZOTINIB | RESISTANCE | OPEN-LABEL | FUSIONS | CHEMOTHERAPY | CHRONIC MYELOID-LEUKEMIA
Journal Article
Tetrahedron Letters, ISSN 0040-4039, 06/2016, Volume 57, Issue 24, pp. 2601 - 2603
This Letter describes the development of a convergent, efficient route to the CHK1 inhibitor MK-8776. This synthetic approach relies upon the cyclization of a... 
Oncology | MK-8776 | CHK1 | Serine/threonine kinase | Kinase | DESIGN | RADIOSENSITIZATION | DNA-DAMAGE RESPONSE | CHEMISTRY, ORGANIC | CANCER | CHECKPOINTS | Pyrimidines
Journal Article
Current Opinion in Investigational Drugs, ISSN 1472-4472, 12/2004, Volume 5, Issue 12, pp. 1311 - 1318
Journal Article
Journal of Medicinal Chemistry, ISSN 0022-2623, 05/2019, Volume 62, Issue 9, pp. 4370 - 4382
PI3K delta catalytic activity is required for immune cell activation, and has been implicated in inflammatory diseases as well as hematological malignancies in... 
SYSTEMIC-LUPUS | PHOSPHOINOSITIDE 3-KINASE DELTA | IN-VITRO | CHEMISTRY, MEDICINAL | PI3K | IDELALISIB | SELECTIVE INHIBITORS | ADENOSINE | CHRONIC LYMPHOCYTIC-LEUKEMIA | INDUCED VASCULAR INJURY | DISCOVERY
Journal Article
Cancer Research, ISSN 0008-5472, 07/2016, Volume 76, Issue 14 Supplement, pp. 2641 - 2641
Introduction: RETPTC1 was one of the first gene fusions identified from a solid tumor. In the past 3 years, oncogenic RET fusions have been identified in... 
Journal Article
Cancer Research, ISSN 0008-5472, 08/2015, Volume 75, Issue 15 Supplement, pp. 791 - 791
Journal Article
Journal Article
Bioorganic and Medicinal Chemistry Letters, ISSN 0960-894X, 01/2011, Volume 21, Issue 1, pp. 467 - 470
Previous efforts by our group have established pyrazolo[1,5-a]pyrimidine as a viable core for the development of potent and selective CDK inhibitors. As part... 
Inhibitors | CHK1 | Kinase | Cell cycle | Pyrazolo[1,5-a]pyrimidine | CDK
Journal Article
Bioorganic and Medicinal Chemistry Letters, ISSN 0960-894X, 01/2011, Volume 21, Issue 1, pp. 471 - 474
The synthesis and hit-to-lead SAR development of a pyrazolo[1,5-a] pyrimidine hit 4 is described leading to a series of potent, selective CHK1 inhibitors such... 
CHK1 | Kinase | Pyrazolo[1,5-a]pyrimidine | Template
Journal Article
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