title: Novel ferrocenyl-containing N-acetyl-2-pyrazolines inhibit in vitro angiogenesis and human lung cancer growth by interfering with F-actin stress fiber polimeryzation.
abstract: Cancer is a significant worldwide health problem generally because of lack of widespread and comprehensive early detection methods. Lung cancer is the leading cause of cancer deaths in men worldwide and the second leading cause of cancer deaths in women. To date, the available treatment regimens are not successful. For this reason, new targets for prevention and new agents for therapy need to be identified. The biological activities of some synthesized ferrocene-containing N-acetylated-2-pyrazoline compounds were studied for this article. Their cytotoxicity (by methyl thiazol tetrazolium assay), as well as apoptotic (by 4'6-diamidino-phenylindole and F-actin staining), antitumoral (colony-forming ability assay) and antiangiogenic activities (by tube formation), were evaluated for the first time on a human non-small-cell lung cancer (A549) cell line and a human umbilicial vein endothelial cell line. All compounds were cytotoxic, antitumoral and apoptotic against tumor cells in a dose-dependent manner. Compounds 2 and 3, which were noncytotoxic, could inhibit capillary vessel formation. Especially, N-acetyl-5-ferrocenyl-3-(2-thienyl)-2-pyrazoline (2) may be used in the development of therapeutic agents for angiogenic diseases and cancer.
authors.affiliation: Department of Biology, Faculty of Science, Anadolu University, Eskişehir, Turkey. beklemb@gmail.com
authors.forename: Rakibe Beklem
authors.initials: RB
authors.lastname: Bostancıoğlu
authors.forename: Seda
authors.initials: S
authors.lastname: Demirel
authors.forename: Günseli
authors.initials: G
authors.lastname: Turgut Cin
authors.forename: Ayse Tansu
authors.initials: AT
authors.lastname: Koparal
mesh_terms: D000199:Actins / Q000378:metabolism*; D020533:Angiogenesis Inhibitors / Q000494:pharmacology*; D000970:Antineoplastic Agents / Q000494:pharmacology*; D017209:Apoptosis / Q000187:drug effects; D045744:Cell Line, Tumor; D003094:Collagen; D003114:Colony-Forming Units Assay; D004305:Dose-Response Relationship, Drug; D004338:Drug Combinations; D005296:Ferrous Compounds / Q000737:chemistry / Q000494:pharmacology*; D061307:Human Umbilical Vein Endothelial Cells; D006801:Humans; D007211:Indoles; D007797:Laminin; D008175:Lung Neoplasms / Q000188:drug therapy*; D009389:Neovascularization, Pathologic / Q000188:drug therapy*; D058105:Polymerization / Q000187:drug effects; D011509:Proteoglycans; D011720:Pyrazoles / Q000737:chemistry / Q000494:pharmacology*; D013778:Tetrazolium Salts; D013844:Thiazoles; D013876:Thiophenes / Q000494:pharmacology*
chemical_list: D000199:Actins; D020533:Angiogenesis Inhibitors; D000970:Antineoplastic Agents; D004338:Drug Combinations; D005296:Ferrous Compounds; D007211:Indoles; D007797:Laminin; C587133:N-acetyl-5-ferrocenyl-3-(2-thienyl)-2-pyrazoline; D011509:Proteoglycans; D011720:Pyrazoles; D013778:Tetrazolium Salts; D013844:Thiazoles; D013876:Thiophenes; C059485:matrigel; C007293:DAPI; D003094:Collagen; C022616:thiazolyl blue