Novel ferrocenyl-containingN-acetyl-2-pyrazolines inhibitin vitroangiogenesis 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.

Anti-angiogenic and antiproliferative properties of the lichen substances (-)-usnic acid and vulpinic acid

“…Thalidomide has been used to inhibit angiogenesis. Bostancioglu et al [28] reported that a concentration of thalidomide as high as 300 μM was required to inhibit tube formation. Thus, (-)-usnic acid at 50 μM and vulpinic acid at 150 μM are more potent than thalidomide.…”

Antitumor effects of deguelin on H460 human lung cancer cells in vitro and in vivo: Roles of apoptotic cell death and H460 tumor xenografts model

“…Lung cancer is the major cause of death in men worldwide and is the second cause of cancer death in women (Bostancioglu et al, ) and it is also happen in Taiwan. Based on the report in 2010 from the Department of Health, R.O.C.…”

Pyrazoles as potential anti-angiogenesis agents: a contemporary overview

“…Recently novel ferrocene-containing N-acetylated-2-pyrazoline compounds were studied for in vitro inhibition of angiogenesis and human lung cancer growth (Bostancioglu et al, 2013). The compounds of interest were synthesized based on bibliographic procedures (see Bostancioglu et al, 2013 and references therein).…”

“…The compounds of interest were synthesized based on bibliographic procedures (see Bostancioglu et al, 2013 and references therein). The final tested products were prepared by reaction of intermediate chalcones with hydrazine hydrate to afford N-acetylated products.…”