Abstract
A series of 1-acyl-1H-[1,2,4]triazole-3,5-diamine analogues were synthesized as cyclin-dependent kinase (CDK) inhibitors. These compounds showed potent and selective CDK1 and CDK2 inhibitory activities and inhibited in vitro cellular proliferation in various human tumor cells. Representative compound 3b demonstrated in vivo efficacy in a human melanoma A375 xenograft model in nude mice.
MeSH terms
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Administration, Oral
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Animals
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Antineoplastic Agents / chemical synthesis*
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Antineoplastic Agents / pharmacokinetics
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Antineoplastic Agents / pharmacology
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Biological Availability
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Cyclin-Dependent Kinases / antagonists & inhibitors*
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Diamines / chemical synthesis*
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Diamines / pharmacokinetics
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Diamines / pharmacology
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Enzyme Inhibitors / chemical synthesis*
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Enzyme Inhibitors / pharmacokinetics
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Enzyme Inhibitors / pharmacology
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Mice
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Mice, Nude
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Molecular Structure
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Rats
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Structure-Activity Relationship
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Triazoles / chemical synthesis*
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Triazoles / pharmacokinetics
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Triazoles / pharmacology
Substances
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Antineoplastic Agents
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Diamines
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Enzyme Inhibitors
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Triazoles
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Cyclin-Dependent Kinases