Novel ferrocenyl-containing N-acetyl-2-pyrazolines inhibit in vitro angiogenesis and human lung cancer growth by interfering with F-actin stress fiber polimeryzation.

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.

1-Acetyl-5-ferrocenyl-3-phenyl-2-pyrazoline.

In the title compound, [Fe(C(5)H(5))(C(16)H(15)N(2)O)], the pyrazoline ring and the phenyl ring are nearly coplanar, making a dihedral angle of 6.54 (2)°, while the substituted cyclo-penta-dienyl ring is twisted out of the pyrazoline ring plane by 81.32 (1)°. The mol-ecules in the crystal structure are held together by weak C-H⋯O inter-molecular hydrogen bonds and two C-H⋯π inter-actions.

Analysis of naturally acquired antibody responses to the 19-kd C-terminal region of merozoite surface protein-1 of Plasmodium vivax from individuals in Sanliurfa, Turkey.

Plasmodium vivax is the second most prevalent global Plasmodium species causing malaria after P. falciparum. These two Plasmodium spp. co-exist in most endemic areas, apart from west and central Africa, which has only P. falciparum. However, southeastern Turkey is one of the exceptional regions with the sole presence of P. vivax infection, where a thorough epidemiologic survey has not been performed. Here, we report for the first time the identification of naturally acquired antibodies against the 19-kd C-terminal region of the merozoite surface protein-1 of P. vivax (PvMSP1(19)), using ELISA, from residents in the Sanliurfa region of southeastern Turkey. Among the 82 samples from patients with patent P. vivax malaria, 85% of the individuals were sero-reactive to PvMSP1(19). Particularly, 69.5% of the subjects were positive for IgM, 53.6% were positive for IgG (predominantly IgG1 and IgG3), and 7.3% were positive for IgA.

1-Acetyl-3-ferrocenyl-5-(2-nitro-phen-yl)-2-pyrazoline.

In the title compound, [Fe(C(5)H(5))(C(16)H(14)N(3)O(3))], the pyrazoline ring and the substituted cyclo-penta-dienyl ring are nearly coplanar, with a dihedral angle of 8.17 (2)°, while the nitro-substituted benzene ring is twisted out of the pyrazoline ring plane by 70.76 (1)°. The mol-ecules in the crystal structure are held together by three inter-molecular C-H⋯O hydrogen bonds. There is also an intra-molecular C-H⋯N hydrogen bond. The H atoms of the methyl group are disordered equally over two positions.