Abstract
(E)- and (Z)-3-Ferrocenylmethylidene-1,3-dihydro-2H-indol-2-ones 1 have been structurally modified in order to explore SAR against a range of kinases. Of note is the submicromolar to low micromolar inhibition of DYRK3 and 4 by a number of complexes. Screening using Xenopus embryos showed some of the compounds to have potent antiangiogenisis activity.
Publication types
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Research Support, Non-U.S. Gov't
MeSH terms
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Animals
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Crystallography, X-Ray
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Embryo, Nonmammalian / drug effects
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Embryo, Nonmammalian / embryology
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Embryo, Nonmammalian / enzymology
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In Situ Hybridization
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Models, Chemical*
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Models, Molecular
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Molecular Structure
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Organometallic Compounds / chemical synthesis*
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Organometallic Compounds / chemistry
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Organometallic Compounds / 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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Structure-Activity Relationship
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Vascular Endothelial Growth Factor Receptor-1 / antagonists & inhibitors
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Vascular Endothelial Growth Factor Receptor-1 / genetics
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Xenopus Proteins / antagonists & inhibitors
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Xenopus Proteins / genetics
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Xenopus laevis / embryology
Substances
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Organometallic Compounds
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Protein Kinase Inhibitors
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Xenopus Proteins
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metallocene
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Vascular Endothelial Growth Factor Receptor-1