Abstract
Hepatocellular carcinoma (HCC) is one of the most common malignancies, yet there have been no significant advances in effective therapeutics. In this study, HS-111 was synthesized as a novel thiazolamine derivative, N-(5-(2-chlorobenzyl) thiazole-2-yl) benzofuran-2-carboxamide, and its anticancer effect and mechanism were examined in human HCC cells. HS-111 strongly suppressed the growth of HCC cells in a dose-dependent manner. Also, apoptosis by HS-111 was identified by DAPI and TUNEL staining, and the increases of the cleaved caspase-3 were observed. In addition, HS-111 decreased protein expression of hypoxia-inducible factor (HIF-1α) and secretion of vascular endothelial growth factor (VEGF), and inhibited tube formation and the migration of human umbilical vein endothelial cells (HUVECs). These results showed that HS-111 not only inhibited cell growth and angiogenesis, but also induced apoptosis of human HCC cells. We suggest that HS-111 may be a potential candidate for chemotherapy against HCC.
Publication types
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Research Support, Non-U.S. Gov't
MeSH terms
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Angiogenesis Inhibitors / chemistry
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Angiogenesis Inhibitors / pharmacology*
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Angiogenesis Inhibitors / therapeutic use
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Apoptosis / drug effects*
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Benzofurans / chemistry
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Benzofurans / pharmacology*
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Benzofurans / therapeutic use
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Blotting, Western
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Carcinoma, Hepatocellular / blood supply
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Carcinoma, Hepatocellular / drug therapy
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Carcinoma, Hepatocellular / pathology*
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Cell Line, Tumor
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Cell Proliferation / drug effects
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Cell Survival / drug effects
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Dose-Response Relationship, Drug
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Enzyme-Linked Immunosorbent Assay
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Human Umbilical Vein Endothelial Cells
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Humans
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In Situ Nick-End Labeling
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Liver Neoplasms / blood supply
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Liver Neoplasms / drug therapy
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Liver Neoplasms / pathology*
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Molecular Structure
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Neovascularization, Pathologic / prevention & control*
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Thiazoles / chemistry*
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Thiazoles / pharmacology
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Thiazoles / therapeutic use
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Wound Healing / drug effects
Substances
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Angiogenesis Inhibitors
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Benzofurans
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N-(5-(2-chlorobenzyl)thiazole-2-yl)benzofuran-2-carboxamide
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Thiazoles