Abstract
Ten novel oleanolic acid (OA) derivatives were synthesized through modifications at positions of A ring and C-28. Inhibitory activities of the oleanolic acid derivatives against SGC7901 and A549 cell lines were evaluated and confirmed by the tetrazolium bromidesalt (MTT) assay. The lab results revealed that all these compounds displayed some antitumor activity against SGC-7901 and A-549 cell lines. Among them, II4 and II5 exhibited excellent antitumor activities against SGC7901 cells and A549 cells, compared with gefitinib. Molecular docking studies have shown that compounds II4 and II5 produce potent antitumor activities by interacting with C-kit receptor through hydrogen bonds and hydrophobic bonds.
Keywords:
Oleanolic acid; antitumor activity; pentacyclic triterpenoid.
MeSH terms
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A549 Cells
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Antineoplastic Agents / chemistry
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Antineoplastic Agents / isolation & purification*
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Antineoplastic Agents / pharmacology*
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Cell Proliferation / drug effects
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Drug Screening Assays, Antitumor
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Gefitinib
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HeLa Cells
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Humans
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Molecular Docking Simulation
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Molecular Structure
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Oleanolic Acid* / analogs & derivatives
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Oleanolic Acid* / chemical synthesis
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Oleanolic Acid* / chemistry
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Oleanolic Acid* / pharmacology
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Pentacyclic Triterpenes / chemistry
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Pentacyclic Triterpenes / isolation & purification*
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Pentacyclic Triterpenes / pharmacology*
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Proto-Oncogene Proteins c-kit / metabolism
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Quinazolines / pharmacology
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Structure-Activity Relationship
Substances
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Antineoplastic Agents
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Pentacyclic Triterpenes
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Quinazolines
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Oleanolic Acid
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Proto-Oncogene Proteins c-kit
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Gefitinib