Abstract
Cyclin-dependent kinases have emerged as important targets for cancer therapy. HSD992, containing a novel scaffold based on the tetrahydro-3H-pyrazolo[4,3-a]phenanthridine core, inhibits CDK2/3 but not other CDKs and also potently inhibits several cancer cell lines.
MeSH terms
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Antineoplastic Agents / chemical synthesis
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Antineoplastic Agents / chemistry
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Antineoplastic Agents / pharmacology*
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Catalytic Domain
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Cell Line, Tumor
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Cyclin-Dependent Kinase 2 / antagonists & inhibitors
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Cyclin-Dependent Kinase 2 / chemistry
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Cyclin-Dependent Kinase 3 / antagonists & inhibitors
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Cyclin-Dependent Kinase 9 / antagonists & inhibitors
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Cyclin-Dependent Kinases / antagonists & inhibitors*
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Cyclin-Dependent Kinases / chemistry
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Drug Evaluation, Preclinical
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Humans
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Molecular Docking Simulation
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Phenanthridines / chemical synthesis
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Phenanthridines / chemistry
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Phenanthridines / pharmacology*
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Protein Kinase Inhibitors / chemical synthesis
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Protein Kinase Inhibitors / chemistry
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Protein Kinase Inhibitors / pharmacology*
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Pyrazoles / chemical synthesis
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Pyrazoles / chemistry
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Pyrazoles / pharmacology*
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Staurosporine / pharmacology
Substances
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Antineoplastic Agents
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Phenanthridines
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Protein Kinase Inhibitors
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Pyrazoles
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CDK2 protein, human
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CDK3 protein, human
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CDK9 protein, human
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Cyclin-Dependent Kinase 2
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Cyclin-Dependent Kinase 3
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Cyclin-Dependent Kinase 9
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Cyclin-Dependent Kinases
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Staurosporine