Abstract
In an attempt to search for new natural product-based antitumor agents, a series of novel (aryl)methyl-amine derivatives of dehydroabietic acid-based B ring-fused-thiazole were designed and synthesized. The primary bioassay showed that compounds 5r and 5s presented certain inhibitory activity against cancer cells, weak cytotoxic activity against normal cells, and inhibitory activity against PI3K/AKT/mTOR signaling pathway. The binding modes and the binding site interactions between the active compounds and the target proteins were predicted preliminarily by the molecular docking method.
Keywords:
Activity; Antitumor; Dehydroabietic acid; Synthesis; Thiazole.
MeSH terms
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Abietanes* / chemistry
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Abietanes* / pharmacology
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Antineoplastic Agents* / chemistry
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Antineoplastic Agents* / pharmacology
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Cell Line, Tumor
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Cell Proliferation / drug effects
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Humans
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Methylamines* / chemistry
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Methylamines* / pharmacology
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Molecular Docking Simulation
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Phosphatidylinositol 3-Kinases / metabolism
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Phosphoinositide-3 Kinase Inhibitors* / chemistry
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Phosphoinositide-3 Kinase Inhibitors* / pharmacology
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Protein Kinase Inhibitors* / chemistry
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Protein Kinase Inhibitors* / pharmacology
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Proto-Oncogene Proteins c-akt / metabolism
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Signal Transduction / drug effects
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TOR Serine-Threonine Kinases / metabolism
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Thiazoles* / chemistry
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Thiazoles* / pharmacology
Substances
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Abietanes
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Antineoplastic Agents
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Methylamines
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Phosphoinositide-3 Kinase Inhibitors
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Protein Kinase Inhibitors
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Thiazoles
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dehydroabietic acid
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Proto-Oncogene Proteins c-akt
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TOR Serine-Threonine Kinases