CIMO - Resumos em Proceedings Não Indexados à WoS/Scopus
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- 1-aryl-3-(4-(7-methylthieno[3,2-d]pyrimidin-4-yloxy)phenyl)ureas: synthesis and molecular modelling studies using VEGFR-2Publication . 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 1-aryl-3-(4-(7-methylthieno[3,2-d]pyrimidin-4-yloxy)phenyl)ureas 2 in high yields by reaction of 4-[(7-methylthieno[3,2-d]pyridin-4-yl)oxy]aniline 1 with arylisocyanates. The former was prepared by regioselective nucleophilic substitution of 4-chloro-7-methylthieno[3,2-d]pyrimidine with 4-aminophenol
- 1-Aryl-3-[ 4-( thieno[3,2-d]pyrimidin-4-yloxy )phenyl]ureas as VEG FR2 inhibitors: synthesis, docking enzymatic and cellular assaysPublication . Peixoto, Daniela; Calhelha, Ricardo C.; Soares, Pedro; Abreu, Rui M.V.; Froufe, Hugo J.C.; Ferreira, Isabel C.F.R.; Costa, Raquel; Soares, Raquel; Queiroz, Maria João R.P.A number of thienopyrimidines derivatives have shown potent VEGFR2 (Vascular Endothelium Growth Factor Receptor2) tyrosine kinase inhibition activity.[ll VEGF is a sun·ogate marker of angiogenesis that activates VEGFR2 in endothelial cells. Here we present the synthesis of new 1-aryl-3-[ 4-(thieno[3,2-d]pyrimidin-4- yloxy)phenyl]ureas from the aminodi(hetero)arylether 1, also prepared by us, which was reacted with arylisocyanates to give the corresponding 1,3-diarylureas 2a-c.
- 1-Aryl-3-[4-(thieno[3,2-d]pyrimidin-4-yloxy)phenyl]ureas as potential inhibitors of VEGFR-2: synthesis and molecular modelling studiesPublication . 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 4-(thieno[3,2-d]pyridin-4-yloxy)aniline 1 which reacts with different arylisocyanates
- 1-Aryl-3-[4-(thieno[3,2-d]pyrimidin-4-yloxy)phenyl]ureas as VEGFR2 tyrosine kinase inhibitors: synthesis, docking studies, enzymatic and cellular assaysPublication . Queiroz, Maria João R.P.; Peixoto, Daniela; Soares, Pedro; Abreu, Rui M.V.; Froufe, Hugo J.C.; Calhelha, Ricardo C.; Ferreira, Isabel C.F.R.; Costa, Raquel; Soares, RaquelA number of thienopyrimidines derivatives have shown potent vascular endothelial growth factor receptor 2 (VEGFR2) inhibition activity. Here, we present the synthesis of new 1-aryl-3-[4-(thieno[3,2-d) pyrimidin-4-yloxy)phenyl]ureas by promoting t he regioselective attack of the hydroxy group of the 4-aminophenol in the chlorine nucleophilic displacement on two 4-chlorinated thieno[3,2-d]pyrimidines, obtaining compounds la and 1b which were reacted with arylisocyanates to give t he corresponding 1,3-diarylureas 2a-f (see scheme). These compounds were evaluated for inhibition of VEGFR2 tyrosine kinase activity using enzymatic assays, and 2a- c showed good inhibition ability with IC50 values in the range of hundreds of nanomolar. The rationale for the inhibition activity is also discussed using docking. To examine the activity of 2a- c in endothelial cells, human umbilical vein endothelial cells (HUVECs) were cultured in the presence or absence of each compound in different concentrations. A decrease in the proliferation of HUVECs was observed by the incorporation of BrdU quantified by ELISA assay. Given the established role of VEGFR2 in proliferation and migration of endothelial cells, these molecules are promising antiangiogenic agents that can be used for therapeutic purposes in pathological conditions where angiogenesis is exacerbated, such as cancer.
- 15 anos de estudo da mosca-da-azeitona, Bactrocera oleae Gmel., no Nordeste de Portugal.Publication . Bento, Albino; Pereira, J.A.A mosca-da-azeitona, Bactrocera oleae (Omel.) e considerada praga chave da oliveira nos países da Bacia do Mediterrâneo, variando a importância dos prejuízos causados pelo insecto consideravelmente entre anos e locais em fun9ao das condi90es climáticas e das políticas agronómicas.
- 2-[(1E,3E)-4-Arylbuta-1,3-dien-1-yl]-4H-chromen-4-ones as dienes in Diels–Alder reactions: experimental and computational studiesPublication . Albuquerque, Hélio; Santos, Clementina M.M.; Lima, Carlos F.R.A.C.; Santos, Luís M.N.B.F.; Cavaleiro, José; Silva, ArturThe synthesis and reactivity of 2-[(1 £,3£)-4-arylbuta-1 ,3-dien-l-yl]-4H-chromen-4-ones 1 as dienes in Diets-Alder (DA) reactions towards several electron-poor and electron-rich dienophiles under microwave irradiation was studied. The optimized reaction conditions were achieved by using N-methylmaleimide2 as dienophile and Sc(0Tf)3 as Lewis acid under microwave-assisted and solvent-free conditions. The Lewis acid improved the reaction yields since it prevented the adducts obtained to undergo a second DA reaction, thus avoiding formation of a bisadduct. The a,~:y ,o-diene of the starting chromones showed to be the most reactive and the computational results confirmed the experimental findings. Theoretical calculations also allowed explaining some unexpected lack of reactivity by some dienophiles. The adducts prepared were dehydrogenated by using DDQ, however, the aza-adducts showed to be sensitive to the high energetic reaction conditions necessary to perform the aromatization.
- 2-Styrylchromones with potencial antioxidant activityPublication . Santos, Clementina M.M.; Silva, Artur; Cavaleiro, José
- 3D tuned porous carbon monolith as catalysts in the wet peroxide oxidation of paracetamolPublication . Roman, Fernanda; Steldinger, Hendryk; Díaz de Tuesta, Jose Luis; Henrique, Adriano; Silva, José A.C.; Gläsel, Jan; Etzold, Bastian J.M.; Gomes, HelderIn recent years, many pharmaceuticals have been identified at trace levels worldwide in the aquatic environment [1]. Municipal wastewater treatment plants (WWTPs) are considered the main sources of these pollutants as they are not generally prepared to deal with such complex substances and thus, they are usually ineffective in their removal [1]. Despite the low concentration of drugs contained in those effluents, the presence of pharmaceuticals, even in trace concentrations, affects the quality of water and constitutes a risk of toxicity for the ecosystems and living organisms [1-2]. Consequently, new regulation for micropollutants discharge and monitoring has been issued in Europe (Directive 2013/39/EU). Paracetamol (PCM) deserves particular attention, since it has recently been discovered as a potential pollutant of waters, largely accumulated in the aquatic environment [3]. This work deals with the treatment of PCM, used as a model pharmaceutical contaminant of emerging concern, by catalytic wet peroxide oxidation using carbon-based monoliths (Fig. 1a) as catalysts. Monoliths were prepared by stereolithographic 3D printing of a photoresin, which was later converted into porous carbon by oxidation in air (300 °C, 6 h) and subsequent pyrolysis in N2 (900 °C, 15 min) as described elsewhere [4]. The materials revealed catalytic activity in the CWPO of PCM allowing to reach PCM conversions up to 30% with a residence time of 3.5 min (Fig. 1b).
- 520b Dynamic prediction of microstructure and molecular size in coordination terpolymerizations including cross-linking and branchingPublication . Dias, Rolando; Costa, Mário RuiThe production of terpolymers using coordination catalysts is a subject with a great industrial importance, being the ethylene-propylene-diene (EPDM) the most representative chemical system within this class of polymers[1-4]. For technical reasons, only a very low content (less than 2 mol %) of diene monomer (such as ethylidene norbornene (ENB)) can usually be incorporated in the terpopolymer. Chain branching and cross-linking, leading eventually to gel formation are important limiting factors to increase the diene content as desired to obtain products with improved properties.
- À descoberta de ecossistemas aquáticos dulçaquícolas: um exemplo de como conciliar turismo e educação/interpretação ambiental.Publication . Geraldes, Ana Maria; Oterino Guillén, Antonio; Salvador Velasco, David; Sheppard, ValerieApesar dos ecossistemas aquáticos dulçaquícolas serem vitais para a humanidade, o seu funcionamento e as espécies que neles habitam são ainda praticamente desconhecidos do grande público. Esta falta de consciencialização limita, em muito, ações que conduzam à sua reabilitação e conservação. Assim, a promoção de atividades de educação e interpretação ambiental inseridas, ou não, em projetos de turismo sustentável, é importante. Nos Parques Naturais do Douro Internacional/Arribes del Duero e do Lago de Sanábria, inseridos na Reserva Transfronteiriça da Meseta Ibérica (MAB_UNESCO), foram implementados dois projetos, únicos, que conciliam atividades turísticas com educação ambiental/ interpretação de ecossistemas aquáticos dulçaquícolas. O promotor é a Estación-Estação Biológica Internacional Duero-Douro, uma organização privada, cuja missão é promover o desenvolvimento sustentável desta região transfronteiriça. O objetivo da presente comunicação é divulgar esta abordagem pouco convencional e inovadora que visa dar a conhecer aspetos do funcionamento e da ecologia dos ecossistemas aquáticos dulçaquícolas, conciliando turismo com educação ambiental. Também serão mencionados trabalhos de investigação, que serão iniciados num futuro próximo, cujo objetivo é avaliar de que forma e em que grau é que estes dois projetos promovem uma maior sensibilização do público participante para a necessidade de conservação destes ecossistemas em particular.