Abstract
A novel metal chelator comprising a 4-(naphthalen-1-yl)pyridine and 2-aminoethanethiol was synthesized. This showed inhibitory activity against human protein farnesyltransferase with IC(50) 1.9 microM, induced morphological change in K-ras-NRK cells at 0.5 microg/mL and showed growth inhibition of K-ras-NRK cells with IC(50) 0.32 microg/mL.
Publication types
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Research Support, Non-U.S. Gov't
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Research Support, U.S. Gov't, P.H.S.
MeSH terms
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Alkyl and Aryl Transferases / antagonists & inhibitors*
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Alkyl and Aryl Transferases / chemistry*
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Animals
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Cell Division / drug effects
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Cell Line
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Chelating Agents / chemical synthesis*
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Chelating Agents / chemistry
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Chelating Agents / pharmacology
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Chlorides / chemistry
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Enzyme Inhibitors / chemical synthesis*
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Enzyme Inhibitors / chemistry
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Enzyme Inhibitors / pharmacology
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Genes, ras / drug effects
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Humans
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Naphthalenes / chemical synthesis*
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Naphthalenes / chemistry
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Naphthalenes / pharmacology
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Pyridines / chemical synthesis*
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Pyridines / chemistry
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Pyridines / pharmacology
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Rats
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Structure-Activity Relationship
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Zinc Compounds / chemistry
Substances
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Chelating Agents
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Chlorides
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Enzyme Inhibitors
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Naphthalenes
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Pyridines
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Zinc Compounds
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zinc chloride
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Alkyl and Aryl Transferases
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p21(ras) farnesyl-protein transferase