8 documents found, page 1 of 1
N-1,2,3-Triazole-Isatin derivatives in lymphoma cell lines
Gaudio, E.; Tarantelli, C.; Marques, C.S.; Ekeh, H.; Carmelo, M.; Burke, A.J.; Bertoni, F.Molecular hybrid constructs are an interesting approach to merge individual pharmacophores with different mechanisms of action, potentially decreasing side effects. The 1,2,3-triazole unit is present in many bioactive compounds and it is characterized by its ability to be stable towards hydrolysis to increase the compounds lipophilicity. Hybrids containing this pharmacophore together with isatin and its analogu...
Survey of New Small Molecule Isatin-based Oxindole Hybrids as Multi-Targeted Dr...
Marques, C.S.; López, O.; Leitzbach, L.; Fernández-Bolaños, J.G.; Stark, H.; Burke, A.J.In the last decade, our group has been very active at developing and assaying complex libraries of scaffolds with a focus on their potential to identify bioactive drug candidates for neurodegenerative diseases, particularly Alzheimer’s disease (AD). Attention has been focused on isatin-based oxindole scaffolds, for which promising results concerning butyrylcholinesterase (BuChE) inhibitory activity have previou...
Evaluation of Chromane Derivatives: Promising Privileged Scaffolds for Lead Dis...
Moutayakine, A.; Marques, C.S.; López, O.; Bagetta, D.; Leitzbach, L.; Hagenow, S.; Carreiro, E.P.; Stark, H.; Alcaro, S.; Fernández-Bolaños, J.G.The chromane ring system is widely distributed in nature and has proven to be a highly potent pharmacophore in medicinal chemistry, which includes the area of Alzheimer’s and Parkinson’s diseases. We report on the development of a gem-dimethylchroman-4-ol family that was shown to give good inhibition of equine serum butyrylcholinesterase (eqBuChE) (in the range 2.9 – 7.3 μM) and in the same range of currently u...
N-1,2,3-Triazole-Isatin Derivatives: Anti-proliferation effects and target iden...
Busto, N.; Leitão-Castro, J.; García-Sosa, A.T.; Cadete, F.; Marques, C.S.; Freitas, R.; Burke, A.J.Molecular hybridization approaches have become an important strategy in medicinal chemistry, and to this end, we have developed a series of novel N-1,2,3-triazole–isatin hybrids that are promising as tumour anti-proliferative agents. Our isatin hybrids presented high cytotoxic activity against colon cancer cell line SW480, lung adenocarcinoma cell line A549, as well as breast cancer cell lines MCF7 and MDA-MB-2...
Isatina: “Bloco de Construção” Promissor no Desenvolvimento de Novos Fármacos
Marques, C.S.; Burke, A.J.A isatina (ou 1H-indole-2,3-diona) é um composto heterocíclico muito cobiçado nas áreas da química medicinal e sintética devido à sua estrutura particularmente versátil no que diz respeito à possibilidade de modificação estrutural e no leque imenso de aplicações que possui. Nos últimos anos tem sido vastamente modificada de forma a provar o seu interesse como potencial fármaco. Neste artigo pretende-se mostrar ...
Sustained drug release by contact lenses for glaucoma treatment - a review
Carvalho, I.M.; Marques, C.S.; Oliveira, Rita; Barata, Pedro; Costa, P.C.; Ferreira, D.C.In the context of ocular pharmacology, there is a growing need for innovative delivery platforms for a convenient and sustained drug release into the eye, especially for chronic diseases that require the adoption of a strict insurmountable treatment regimen for a large part of the affected population, as in the case of glaucoma. Due to the large residence time of the contact lenses in the eye, its use for susta...
Papel do Licopeno na melhoria da Qualidade de Vida
Marques, C.S.; Lima, Maria João Reis; Oliveira, Jorge; Lemos, Edite Teixeira deA escolha da nutrição mais adequada tem sido um tema estudado com grande interesse ao longo da história da humanidade tendo em conta a manutenção da Saúde, mas igualmente com outras finalidades como o atraso do envelhecimento ou outros benefícios. O desafio colocado pela ingestão de frutos, vegetais, cereais, azeite e vinho aplicado pela intitulada Dieta Mediterrânica torna possível o entendimento de países com...
Tomato Lycopene: Functional Proprieties and Health
Marques, C.S.; Lima, Maria João Reis; Oliveira, J.; Lemos, Edite Teixeira deThe growing concerns for physical wellbeing and health have been reflected in the way we choose food in our table. Nowadays, we are all more informed consumers and choose healthier foods. On the other hand, stroke, cancer and atherosclerosis may be somehow minimized by the intake of some bioactive compounds present in food, the so-called nutraceuticals and functional foods. The aim of this work was to make a re...