163 research outputs found

    Novel 1,4-benzoxazine and 1,4-benzodioxine inhibitors of angiogenesis.

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    Esters of 1,4-benzoxazine and 1,4-benzodioxine compounds 1 and 10, which combine thrombin inhibitory and GPIIb/IIIa antagonistic activity in one molecule are shown to inhibit endothelial cell migration and tube formation in vitro and angiogenesis in the chicken chorioallantoic membrane (CAM) assay. The corresponding carboxylic acids 1 (R2 = H) and 11 were devoid of antiangiogenic activity, most probably due to their insufficient entry into the cell. Although thrombin inhibition remains the most probable explanation for their inhibition of angiogenesis, VEGFR2 kinase assay suggest that other targets such as VEGFR2 might be involved

    Highly functionalized 2-oxopiperazine-based peptidomimetics: An approach to PAR1 antagonists

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    A series of pseudodipeptide-based chiral 1,3,4,5-tetrasubstituted-2- oxopiperazines has been designed and synthesized as potential PAR1 antagonists. These highly functionalized piperazines were synthesized from aromatic and basic amino acid derived Ψ[CH(CN)NH]pseudodipeptides through a four step pathway that involves reduction of the cyano group to build the 2-oxopiperazine ring, followed by selective functionalization at the N4-, N 1-positions, and at the exocyclic moiety at position C5. This regioselective functionalization required the fine tuning of reaction conditions. All new compounds were screened as inhibitors of human platelet aggregation induced by the PAR1 agonist SFLLRN and as cytotoxic agents in human cancer cell lines. Some of the compounds displayed moderate PAR1 antagonist activity, while, others were cytotoxic at μM concentration. No correlation was observed between both types of activities.Peer Reviewe

    Evaluation of Greenhouse Gas Emissions of Quinoa Seed Production in Greece

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    Population growth has led to an increase in food production, resulting in an increase in agricultural products in terms of quantity and quality. Quinoa (Chenopodium quinoa Willd.) cultivation is prevalent in most areas of the world due to its high-quality grain and its potential to produce high yields under tough growing conditions. This study aimed to investigate all greenhouse gas (GHG) emissions generated by quinoa seed production in Greece and their relationship with farm-related factors, from fertilizer production to energy consumption for all cultivation techniques. The amount of all GHG emissions was estimated using Cool Farm Tool software. In order to collect data, a questionnaire including questions regarding cultivation details, soil characteristics, inputs, fuel, and water use was distributed and completed by forty quinoa producers from Central Greece. Accordingly, the estimated carbon footprint values per hectare and per kilogram of quinoa seed were 1,159.65 and 0.48 kg CO2-eq, respectively. The present research also found that the highest CO2-eq emissions per kilogram of quinoa seed were found to be associated with the production of fertilizers, with a value of 0.20 kg CO2-eq corresponding to 40.88% of the total emissions per kilogram of produced seed. Consequently, attention must be given for the mitigation of the environmental impact of quinoa seed production. It is particularly important to manage chemical fertilizers and agricultural machinery properly in order to ensure the sustainable cultivation of quinoa

    Performance of two cotton interspecific hybrids (Gossypium hirsutum L. × G. barbadense L.) in Greece: A comparative case study

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    Cotton (Gossypium hirsutum L.) is one of the most prominent and important industrial crops. In Greece, cotton farming occupies a significant share of the agricultural sector. However, the adverse effects of climate change have raised concerns regarding its performance in the near future, thus it is crucial to develop adaptation strategies for the production of cotton in Greece. One such alternative is the adoption of interspecific hybrids (G. hirsutum × G. barbadense). These hybrids have been suggested to be more resilient and to outperform their parental varieties. In order to evaluate the potential of such hybrids, a field experiment was conducted in two sites in Greece. Two novel cotton hybrids (1432 and 701) and a conventional variety (‘Elpida’) were farmed in two different plant densities (8 and 13 plants m2) and their agronomic traits (biomass, LAI), yield and yield components (seed cotton yield, lint yield, seed yield, ration lint/seed cotton, and ratio seed/seed cotton), and quality traits were assessed. The agronomic traits and the yield of the hybrids were equal or superior in comparison to ‘Elpida’. Similar findings were also observed in the majority of the quality traits. Based on our results, interspecific cotton hybrids are promising for the European cotton sector. 

    Molecular biology of breast cancer metastasis Molecular expression of vascular markers by aggressive breast cancer cells

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    During embryogenesis, the formation of primary vascular networks occurs via the processes of vasculogenesis and angiogenesis. In uveal melanoma, vasculogenic mimicry describes the 'embryonic-like' ability of aggressive, but not nonaggressive, tumor cells to form networks surrounding spheroids of tumor cells in three-dimensional culture; these recapitulate the patterned networks seen in patients' aggressive tumors and correlates with poor prognosis. The molecular profile of these aggressive tumor cells suggests that they have a deregulated genotype, capable of expressing vascular phenotypes. Similarly, the embryonic-like phenotype expressed by the aggressive human breast cancer cells is associated with their ability to express a variety of vascular markers. These studies may offer new insights for consideration in breast cancer diagnosis and therapeutic intervention strategies
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