Abstract
A series of 4-amino-6-piperazin-1-yl-pyrimidine-5-carbaldehyde oximes has been discovered and developed as potent FLT3 tyrosine kinase inhibitors. The series exhibited potent antiproliferative activity against both an FLT3 ITD-mutated human leukemic cell line as well as a wild-type FLT3 BaF(3) expressed cell line. The structure-activity relationship of this class of compounds is described.
MeSH terms
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Aldehydes / chemistry*
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Cell Line, Tumor
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Cell Proliferation
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Chemistry, Pharmaceutical / methods*
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Drug Design
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Drug Screening Assays, Antitumor
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Humans
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Inhibitory Concentration 50
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Models, Chemical
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Mutation
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Oximes / chemical synthesis*
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Oximes / chemistry
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Oximes / therapeutic use*
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Structure-Activity Relationship
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fms-Like Tyrosine Kinase 3 / antagonists & inhibitors*
Substances
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Aldehydes
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Oximes
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FLT3 protein, human
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fms-Like Tyrosine Kinase 3