Abstract
Tumor growth and metastasis are highly associated with the overexpression of protein kinases (PKs) regulating cell growth, apoptosis resistance, and prolonged cell survival. This study describes novel azaindolyl-maleimides with significant inhibition of PKs, such as VEGFR, FLT-3, and GSK-3β which are related to carcinogenesis. Furthermore, these compounds exhibit high kinase selectivity and potent inhibition of angiogenesis and cell proliferation, offering versatile options in cancer treatment strategies.
Publication types
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Research Support, Non-U.S. Gov't
MeSH terms
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Angiogenesis Inhibitors / pharmacology*
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Animals
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Apoptosis / drug effects
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Cell Cycle / drug effects
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Cell Proliferation / drug effects*
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Cells, Cultured
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Chick Embryo
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Glycogen Synthase Kinase 3 / antagonists & inhibitors
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Glycogen Synthase Kinase 3 beta
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Growth Inhibitors / pharmacology*
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Human Umbilical Vein Endothelial Cells / drug effects
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Humans
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Maleimides / chemistry*
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Molecular Structure
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Neoplasms / drug therapy*
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Neovascularization, Pathologic / drug therapy*
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Protein Kinase Inhibitors / pharmacology*
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Structure-Activity Relationship
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Vascular Endothelial Growth Factor Receptor-2 / antagonists & inhibitors
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Vascular Endothelial Growth Factor Receptor-3 / antagonists & inhibitors
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fms-Like Tyrosine Kinase 3 / antagonists & inhibitors
Substances
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Angiogenesis Inhibitors
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Growth Inhibitors
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Maleimides
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Protein Kinase Inhibitors
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maleimide
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FLT3 protein, human
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Vascular Endothelial Growth Factor Receptor-2
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Vascular Endothelial Growth Factor Receptor-3
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fms-Like Tyrosine Kinase 3
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GSK3B protein, human
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Glycogen Synthase Kinase 3 beta
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Glycogen Synthase Kinase 3