Abstract
Inspired by bioactive indoline alkaloid natural products, here, we report a divergent synthesis approach that led to skeletally diverse indoline alkaloid-inspired compounds. The natural product-inspired compounds obtained were then subjected to a series of in vitro and cellular assays to examine their properties as modulators of focal adhesion kinase (FAK) activity. This study resulted in the identification of a promising lead inhibitor of FAK (42), which also showed activity in a wound healing and cell invasion assay. The in silico study of the lead compound (42) was also undertaken.
Publication types
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Research Support, Non-U.S. Gov't
MeSH terms
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Breast Neoplasms / drug therapy
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Breast Neoplasms / metabolism
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Breast Neoplasms / pathology
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Cell Adhesion / drug effects
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Cell Movement / drug effects
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Cell Proliferation / drug effects
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Computer Simulation
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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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Female
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Focal Adhesion Protein-Tyrosine Kinases / antagonists & inhibitors*
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Humans
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Indole Alkaloids / chemical synthesis
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Indole Alkaloids / chemistry
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Indole Alkaloids / pharmacology*
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Indoles / chemical synthesis
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Indoles / chemistry
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Indoles / pharmacology*
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Phosphorylation / drug effects
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Signal Transduction / drug effects*
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Tumor Cells, Cultured
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Wound Healing / drug effects
Substances
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Enzyme Inhibitors
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Indole Alkaloids
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Indoles
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indoline
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Focal Adhesion Protein-Tyrosine Kinases