Back to Search
Start Over
4-(1H-Indazol-5-yl)-6-phenylpyrimidin-2(1H)-one analogs as potent CDC7 inhibitors
- Source :
- Bioorganic & Medicinal Chemistry Letters. 18:4482-4485
- Publication Year :
- 2008
- Publisher :
- Elsevier BV, 2008.
-
Abstract
- A series of 4-(4-hydroxyphenyl)-6-phenylpyrimidin-2(1H)-ones were identified by HTS as inhibitors of CDC7. Molecular modeling and medicinal chemistry techniques were employed to explore the SAR for this series with a focus on removing potential metabolic liabilities and improving cellular potency.
- Subjects :
- Indazoles
Molecular model
Stereochemistry
Chemistry, Pharmaceutical
Clinical Biochemistry
Molecular Conformation
Pharmaceutical Science
Cell Cycle Proteins
Pyrimidinones
Non-specific serine/threonine protein kinase
Protein Serine-Threonine Kinases
Biochemistry
Inhibitory Concentration 50
Structure-Activity Relationship
chemistry.chemical_compound
Drug Discovery
Humans
Pyrimidone
Enzyme Inhibitors
Molecular Biology
chemistry.chemical_classification
Indazole
Binding Sites
Molecular Structure
Bicyclic molecule
biology
Organic Chemistry
Enzyme
Models, Chemical
chemistry
Enzyme inhibitor
Drug Design
Benzene derivatives
biology.protein
Molecular Medicine
Caco-2 Cells
Subjects
Details
- ISSN :
- 0960894X
- Volume :
- 18
- Database :
- OpenAIRE
- Journal :
- Bioorganic & Medicinal Chemistry Letters
- Accession number :
- edsair.doi.dedup.....217a9c193aa9d3505e5bd2a9da18d9e6
- Full Text :
- https://doi.org/10.1016/j.bmcl.2008.07.061