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Registros recuperados: 55 | |
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Soares, Pedro; Froufe, Hugo J.C.; Abreu, Rui M.V.; Ferreira, Isabel C.F.R.; Borges, Fernanda; Queiroz, Maria João R.P.. |
The development of anticancer drugs inhibiting angiogenesis has been an area of extensive research in the past decade. Angiogenesis is a requirement for tumor growth and metastasis and occurs through several signalling pathways. One key pathway that initiates proliferation and migration of endothelial cells is signalling through the vascular endothelial growth factor receptor-2 (VEGFR-2).1 Therefore, small molecules that block this signalling pathway through inhibition of VEGFR-2 tyrosine kinase activity could potentially inhibit angiogenesis and tumor growth. Recently works describing thienopyrimidine2 and thienopyrimidine 1,3-diarylureas3 as VEGFR-2 inhibitors have emerged in the literature. Here we present the synthesis of new... |
Tipo: ConferenceObject |
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Ano: 2011 |
URL: http://hdl.handle.net/10198/6079 |
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Soares, Pedro; Froufe, Hugo J.C.; Abreu, Rui M.V.; Ferreira, Isabel C.F.R.; Borges, Fernanda; Queiroz, Maria João R.P.. |
Angiogenesis is a requirement for tumor growth and metastasis and occurs through several signalling pathways. One key pathway that initiates proliferation and migration of endothelial cells is signalling through the vascular endothelial growth factor receptor-2 (VEGFR-2).1 Therefore, small molecules that block this signalling pathway through inhibition of the VEGFR tyrosine kinase activity could potentially inhibit angiogenesis and tumour growth. Recently works describing thienopyrimidines2 and thienopyridine ureas3 as inhibitors of VEGFR-2 have appeared in the literature. Here we present the synthesis of new 1,3-diarylureas 2 starting by regioselective nucleophilic substitution of the 4-chlorothieno[3,2-d]pyrimidine with 4-aminophenol to obtain... |
Tipo: ConferenceObject |
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Ano: 2011 |
URL: http://hdl.handle.net/10198/6077 |
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Ferreira, Isabel C.F.R.; Queiroz, Maria João R.P.; Barros, Lillian; Abreu, Ana S.; Ferreira, Paula M.T.. |
Free radical formation is associated with the normal natural metabolism of aerobic cells. The oxygen consumption inherent to cell growth leads to the generation of a series of oxygen free radicals. The interaction of these species with lipid molecules produces new radicals that may interact with biological systems in a cytotoxic manner. Free radicals and their uncontrolled production are responsible for several pathological processes, such as certain tumours (prostate and colon cancers) the reducing properties of diarylamines make them very important as antioxidants, especially as radical scavengers. |
Tipo: ConferenceObject |
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Ano: 2007 |
URL: http://hdl.handle.net/10198/3720 |
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Abreu, Rui M.V.; Froufe, Hugo J.C.; Daniel, Pedro O.M.; Queiroz, Maria João R.P.; Ferreira, Isabel C.F.R.. |
Mushrooms represent an unlimited source of compounds with antitumor and immunostimulating properties and mushroom intake as been shown to reduce the risk of breast cancer. A large number of LMW (low molecular weight) compounds present in mushrooms have been identified including: phenolic acids, flavonoids, tocopherols, carotenoids, sugars and fatty acids. In order to evaluate which wild mushroom LMW compounds may be involved in anti-breast cancer activity we selected a representative dataset of 43 LMW compounds and performed molecular docking against 3 known protein targets involved in breast cancer (Aromatase, Estrone Sulfatase and 17β-HSD-1) using AutoDock4 as docking software. The estimated inhibition constants for all LMW compounds were determined and... |
Tipo: Article |
Palavras-chave: Mushrooms; Nutraceuticals; Breast cancer; Molecular Docking; AutoDock4. |
Ano: 2011 |
URL: http://hdl.handle.net/10198/6231 |
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Abreu, Rui M.V.; Froufe, Hugo J.C.; Queiroz, Maria João R.P.; Ferreira, Isabel C.F.R.. |
O desenvolvimento de novas ferramentas computacionais é uma parte integral da área da bioinformática. A disponibilização destas ferramentas em modalidade de acesso livre permitir o acesso a um maior número de utilizadores e facilita significativamente o seu desenvolvimento pela facilidade de troca de ideias entre utilizadores. Neste trabalho, serão apresentados dois softwares desenvolvidos pelo nosso grupo de investigação: 1) MOLA1 que automatiza o screening virtual de bibliotecas de compostos com baixa massa molar, utilizando as ferramentas de docking AutoDock4 e AutoDock Vina; 2) ChemT2 que permite a geração de bibliotecas de compostos análogos de baixa massa molar, tendo como base uma estrutura química de interesse. Será ainda apresentado um exemplo de... |
Tipo: ConferenceObject |
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Ano: 2011 |
URL: http://hdl.handle.net/10198/6072 |
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Martins, M.A.; Ferreira, Isabel C.F.R.; Santos, I.M.; Queiroz, Maria João R.P.; Lima, Nelson. |
Sintetizaram-se corantes azo de aplicação têxtil, usando como componentes diazo ácidos aminobenzóicos e arrunossulfónicos e como componentes de acoplamento 2.metoxifenol e 2,6-dimetoxifenoL A utilização destas componentes de acoplamento !tve como objectivo aumentar a bioacessibilidade dos corantes ao fungo lenhinolítico da podridão branca Phanerochaete chrysosporium, já que estes grupos estão presentes na estrutura da lenhina e têm sido referidos como pontos de acesso para o sistema enzimático lenhinolítico do fungo. As experiências de biodegradação realizaram-se em meio líquido. com sacarose e em condições limitantes de azoto, com agitação e !tmperatura controladas. A biodegradação dos corantes foi acompanhada por espec trofotometria UV-Visível,... |
Tipo: ConferenceObject |
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Ano: 1999 |
URL: http://hdl.handle.net/10198/3875 |
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Ferreira, Isabel C.F.R.; Queiroz, Maria João R.P.; Vilas-Boas, Miguel; Estevinho, Leticia M.; Begouin, Agathe; Kirsch, Gilbert. |
The antioxidant properties of substituted diarylamines in the benzo[b]thiophene series were evaluated by their reducing power and free radical scavenging activity. The results were compared with those of standards: acid ascorbic for the first method and BHA and BHT for the second. For both methods it was possible to establish some structure–activity relationships (SARs) based on the position of the arylamination on the benzo[b]thiophene moiety, the presence of different substituents on the phenyl ring (F, 1 or 2 OMe) and on the thiophene ring (H, CO2Et, CO2H). |
Tipo: Article |
Palavras-chave: Diarylamines; Benzothiophenes; Antioxidant activity; Structure–activity relationships. |
Ano: 2006 |
URL: http://hdl.handle.net/10198/825 |
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Abreu, Rui M.V.; Falcão, Soraia; Ferreira, Isabel C.F.R.; Queiroz, Maria João R.P.; Vilas-Boas, Miguel. |
Cyclic voltammetry was used to evaluate the antioxidant activity of 7-aryl or 7-heteroarylamino-2,3-dimethylbenzo[b]thiophenes previously synthesized by some of us, comparing their oxidation potentials with those of the well-known synthetic standards (BHA, BHT). Compounds with electron-donating groups on the arylamine moiety have lower Ep/2 than compounds with electron-withdrawing groups or electron-deficient rings (pyridines). The position of the methoxy group on the arylamine moiety also changes the oxidation potential: lower Ep/2 for the diarylamines with methoxy groups in the para position. Comparing the first peak potential with the ones of BHA and BHT, the diarylamine compounds show lower oxidation potential, and therefore higher reducing power. A... |
Tipo: Article |
Palavras-chave: Benzo[b]thiophene; Diarylamines; Antioxidant properties; Electrochemical assays. |
Ano: 2009 |
URL: http://hdl.handle.net/10198/2717 |
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Ferreira, Isabel C.F.R.; Barros, Lillian; Falcão, Soraia; Vilas-Boas, Miguel; Queiroz, Maria João R.P.. |
The skin provides the first line of defense against oxidative damage induced by environmental factors, having an elaborated antioxidant system designed to deal with free radicals and oxidative stress. However, under severe stress conditions this biological response is not sufficient, leading to oxidative damage and, in consequence, to skin disorders, immunosuppresion, premature skin aging and ultimately cancer. |
Tipo: ConferenceObject |
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Ano: 2007 |
URL: http://hdl.handle.net/10198/3715 |
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Peixoto, Daniela; Calhelha, Ricardo C.; Dias, Sofia; Froufe, Hugo J.C.; Abreu, Rui M.V.; Ferreira, Isabel C.F.R.; Queiroz, Maria João R.P.. |
When over expressed or mutated, protein tyrosine kinases become potent oncoproteins that cause deregulated cell growth angiogenesis and metastasis. Because of these characteristics, they are targets for small molecule inhibitors in the treatment of cancer. Recently some thieno[3,2-c]pyridine 1,3-diarylurea derivatives were prepared as VEGFR-2 (vascular endothelium growth factor receptor-2) inhibitors.1 Here we present the synthesis of methyl 3-[4-(3-arylureido)phenylamino]thieno[3,2-b]pyridine-2-carboxylates 2 in excellent yields, by reaction of the methyl 3-(4-aminophenylamino)thieno[3,2-b]pyridine-2-carboxylate 1, prepared also by us, with different arylisocyanates (Scheme). |
Tipo: ConferenceObject |
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Ano: 2011 |
URL: http://hdl.handle.net/10198/6006 |
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Registros recuperados: 55 | |
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