Abstract
Hybrid molecules have been developed which are comprised of a tyrosine kinase-targeted, quinazoline-based scaffold and a flexibly linked dia(m)minechloridoPt(ii) moiety. The target compounds maintain high affinity and selectivity for ErbB family kinase proteins and one of the derivatives induces platinum adducts with a pharmacologically important cysteine residue.
MeSH terms
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Amino Acid Sequence
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Catalytic Domain
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Coordination Complexes / chemical synthesis
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Coordination Complexes / metabolism*
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Cysteine / chemistry*
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ErbB Receptors / antagonists & inhibitors
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ErbB Receptors / chemistry
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ErbB Receptors / metabolism*
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Humans
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Organoplatinum Compounds / chemical synthesis
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Organoplatinum Compounds / metabolism*
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Platinum / chemistry*
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Protein Binding
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Protein Kinase Inhibitors / chemical synthesis
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Protein Kinase Inhibitors / metabolism
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Quinazolines / chemical synthesis
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Quinazolines / metabolism*
Substances
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Coordination Complexes
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Organoplatinum Compounds
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Protein Kinase Inhibitors
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Quinazolines
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Platinum
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EGFR protein, human
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ErbB Receptors
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Cysteine