Cytotoxic effect of a novel synthesized carbazole compound on A549 lung cancer cell line

Increased death rates due to lung cancer have necessitated the search for potential novel anticancer compounds such as carbazole derivatives. Carbazoles are aromatic heterocyclic compounds with anticancer, antibacterial and anti-inflammatory activity. The study investigated the ability of the novel carbazole compound (Z)-4-[9-ethyl-9aH-carbazol-3-yl) amino] pent-3-en-2-one (ECAP) to induce cytotoxicity of lung cancer cells and its mechanism of action. ECAP was synthesized as a yellow powder with melting point of 240-247 °C. The 3-(4,5-dimethythiazol-2-yl)-2,5-diphenyl tetrazolium bromide (MTT), lipid peroxidation and comet assays were used to assess the cytotoxic effect of the compound on A549 lung cancer cells. Protein expression was determined using western blots, apoptosis was measured by luminometry (caspase-3/7, -8 and -9) assay and flow cytometry was used to measure phosphatidylserine (PS) externalisation. ECAP induced a p53 mediated apoptosis of lung cancer cells due to a significant reduction in the expression of antioxidant defence proteins (Nrf2 and SOD), Hsp70 (p < 0.02) and Bcl-2 (p < 0.0006), thereby up-regulating reactive oxygen species (ROS) production. This resulted in DNA damage (p < 0.0001), upregulation of Bax expression and caspase activity and induction of apoptosis in lung cancer cells. The results show the anticancer potential of ECAP on lung cancer.S1 Fig. MTT assay measured in untreated (control) and 1% DMSO (vehicle control) treated A549 cells. The data showed no significant cytotoxicity.S2 Fig.Western blots showing the effect of ECAP on the expression of Bax, Bcl-2, p53, Nrf2, Hsp70 and SOD. The original western blots which were used for western blot analysis (Fig 6).College of Health Sciences, University of KwaZulu-Natalhttp://www.plosone.orgam201

Vilsmeier-Haack reaction: A manifest protocol to synthesise bisquinoline

517-521<span style="font-size:11.0pt;font-family: " times="" new="" roman";mso-fareast-font-family:"times="" roman";mso-bidi-font-family:="" mangal;mso-ansi-language:en-gb;mso-fareast-language:en-us;mso-bidi-language:="" hi"="" lang="EN-GB">Synthesis of bisquinolines from methyl anthranilate and ethyl acetoacetate is described. This synthesis has been accomplished in three steps. Vilsmeier-Haack reaction is used as a key tool to assemble bisquinoline. Microwave heating during each step of the reaction gives high yield of products in short reaction times.</span

A one pot microwave assisted synthesis of 3-acyl-2,4-dihydroxyquinoline followed by synthesis of 7-methyldibenzo[<i style="mso-bidi-font-style:normal">c</i>,<i style="mso-bidi-font-style:normal">f</i>][2,7]naphthyridin-6(5<i style="mso-bidi-font-style:normal">H</i>)-ones <i style="mso-bidi-font-style:normal">via</i> three routes

776-786An easy one pot microwave assisted synthesis of 3-acyl-2,4-dihydroxyquinoline from simple precursors followed by convenient synthesis of novel and potential HIV integrase inhibitors 7-methyldibenzo[c,f][2,7]naphthyridin-6(5H)-ones has been achieved through three different routes. Mild reaction conditions and good yields are obtained by applying microwave and photochemical techniques

Studying Fischer–Tropsch catalysts using transmission electron microscopy and model systems of nanoparticles on planar supports

Nanoparticle model systems on planar supports form a versatile platform for studying morphological and compositional changes of catalysts due to exposure to realistic reaction conditions. We review examples from our work on iron and cobalt catalysts, which can undergo significant rearrangement in the reactive environment of the Fischer–Tropsch synthesis. The use of specially designed, silicon based supports with thin film SiO2 enables the application of transmission electron microscopy, which has furnished important insight into e.g. the mechanisms of catalyst regeneration