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Discovery of a novel class of triazolones as Checkpoint Kinase inhibitors—Hit to lead exploration
- Source :
- Bioorganic & Medicinal Chemistry Letters. 20:5133-5138
- Publication Year :
- 2010
- Publisher :
- Elsevier BV, 2010.
-
Abstract
- Checkpoint Kinase-1 (Chk1, CHK1, CHEK1) is a Ser/Thr protein kinase that mediates cellular responses to DNA-damage. A novel class of Chk1 inhibitors, triazoloquinolones/triazolones (TZ's) was identified by high throughput screening. The optimization of these hits to provide a lead series is described.
- Subjects :
- Models, Molecular
animal structures
High-throughput screening
genetic processes
Clinical Biochemistry
Pharmaceutical Science
Computational biology
Crystallography, X-Ray
environment and public health
Biochemistry
Structure-Activity Relationship
Drug Discovery
Structure–activity relationship
CHEK1
Protein kinase A
Protein Kinase Inhibitors
Molecular Biology
Kinase
Drug discovery
Chemistry
Organic Chemistry
Hit to lead
Triazoles
enzymes and coenzymes (carbohydrates)
Checkpoint Kinase 1
Molecular Medicine
biological phenomena, cell phenomena, and immunity
Signal transduction
Protein Kinases
Subjects
Details
- ISSN :
- 0960894X
- Volume :
- 20
- Database :
- OpenAIRE
- Journal :
- Bioorganic & Medicinal Chemistry Letters
- Accession number :
- edsair.doi.dedup.....02edc1c68b5470ccac027b686d298564