Structure-based drug design of a highly potent CDK1,2,4,6 inhibitor with novel macrocyclic quinoxalin-2-one structure
Copyright policy )Structure-based drug design of a highly potent CDK1,2,4,6 inhibitor with novel macrocyclic quinoxalin-2-one structure
The design of a novel series of cyclin-dependent kinase (CDK) inhibitors containing a macrocyclic quinoxaline-2-one is reported. Structure-based drug design and optimization from the starting point of diarylurea 2, which we previously reported as a moderate CDK1,2,4,6 inhibitor [J. Biol.Chem.2001, 276, 27548], led to the discovery of potent CDK1,2,4,6 inhibitor that were suitable for iv administration for in vivo study.
- Merck & Co. United States
Binding Sites, Macrocyclic Compounds, Molecular Structure, Cyclin-Dependent Kinase 2, Cyclin-Dependent Kinase 4, Hydrogen Bonding, Cyclin-Dependent Kinase 6, Crystallography, X-Ray, Inhibitory Concentration 50, Structure-Activity Relationship, Drug Design, Quinoxalines, CDC2 Protein Kinase, CDC2-CDC28 Kinases, Animals, Humans
Binding Sites, Macrocyclic Compounds, Molecular Structure, Cyclin-Dependent Kinase 2, Cyclin-Dependent Kinase 4, Hydrogen Bonding, Cyclin-Dependent Kinase 6, Crystallography, X-Ray, Inhibitory Concentration 50, Structure-Activity Relationship, Drug Design, Quinoxalines, CDC2 Protein Kinase, CDC2-CDC28 Kinases, Animals, Humans
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