title: The effect of HS-111, a novel thiazolamine derivative, on apoptosis and angiogenesis of hepatocellular carcinoma cells.
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.
authors.affiliation: Department of Biomedical Sciences and Clinical Research Center, College of Medicine, Inha University, Incheon, 400-712, Korea.
authors.forename: Myung-Joo
authors.initials: MJ
authors.lastname: Choi
authors.forename: Hyunseung
authors.initials: H
authors.lastname: Lee
authors.forename: Ju-Hee
authors.initials: JH
authors.lastname: Lee
authors.forename: Kyung Hee
authors.initials: KH
authors.lastname: Jung
authors.forename: Donghee
authors.initials: D
authors.lastname: Kim
authors.forename: Sungwoo
authors.initials: S
authors.lastname: Hong
authors.forename: Soon-Sun
authors.initials: SS
authors.lastname: Hong
mesh_terms: D020533:Angiogenesis Inhibitors / Q000737:chemistry / Q000494:pharmacology* / Q000627:therapeutic use; D017209:Apoptosis / Q000187:drug effects*; D001572:Benzofurans / Q000737:chemistry / Q000494:pharmacology* / Q000627:therapeutic use; D015153:Blotting, Western; D006528:Carcinoma, Hepatocellular / Q000098:blood supply / Q000188:drug therapy / Q000473:pathology*; D045744:Cell Line, Tumor; D049109:Cell Proliferation / Q000187:drug effects; D002470:Cell Survival / Q000187:drug effects; D004305:Dose-Response Relationship, Drug; D004797:Enzyme-Linked Immunosorbent Assay; D061307:Human Umbilical Vein Endothelial Cells; D006801:Humans; D020287:In Situ Nick-End Labeling; D008113:Liver Neoplasms / Q000098:blood supply / Q000188:drug therapy / Q000473:pathology*; D015394:Molecular Structure; D009389:Neovascularization, Pathologic / Q000517:prevention & control*; D013844:Thiazoles / Q000737:chemistry* / Q000494:pharmacology / Q000627:therapeutic use; D014945:Wound Healing / Q000187:drug effects
chemical_list: D020533:Angiogenesis Inhibitors; D001572:Benzofurans; C574711:N-(5-(2-chlorobenzyl)thiazole-2-yl)benzofuran-2-carboxamide; D013844:Thiazoles