37 documents found, page 1 of 4
Targeting Vascular Endothelial Growth Factor Receptor 2 (VEGFR-2): Latest Insig...
Marques, Carolina S.; Brandão, Pedro; Burke, Anthony J.Vascular endothelial growth factor receptor 2 (VEGFR-2) is a crucial mediator of angiogene- sis, playing a pivotal role in both normal physiological processes and cancer progression. Tumors harness VEGFR-2 signaling to promote abnormal blood vessel growth, which is a key step in the metastasis process, making it a valuable target for anticancer drug development. While there are VEGFR-2 inhibitors approved for t...
Book of Abstracts, International Symposium on Synthesis & Catalysis 2023
Marques, Carolina S.; Carreiro, Elisabete P.; Burke, Anthony J.On behalf of the Organizing Committee I am very pleased to welcome you to the fifth edition of the International Symposium on Synthesis and Catalysis (ISySyCat2023) once again at the historic University of Évora. The inaugural edition of this conference that took place in September 2015 (ISySyCat2015) was a great success and from that moment we have been building on this success, making this a regular biannual ...
Chitosan Salts as Stabilizing Agents for the synthesis of Silver Nanoparticles ...
Carreiro, Elisabete P.; Teixeira, António P.S.; Costa, Marina; Burke, Anthony J.; Filho, Cesar; Gonçalves, Isabel; Craveiro, Alexandre; Silva, MaraIn this work, silver nanoparticles (AgNPs) were obtained by a chemical reduction method using different chitosan salts as stabilizing agents, able to protect and prevent against the aggregation of the nanoparticles. Various chitosan salts with different organic acids, which included: acetic, succinic, formic, propionic, malic, glycolic and lactic acid were used to form the chitosan salts. The use of these organ...
Easy access to Ugi-derived Isatin-peptoids and their potential as small-molecul...
Marques, Carolina S.; González-Bakker, Aday; Padrón, José M.; Burke, Anthony J.An amide bond is one of the most important functional motifs in chemistry and biology due to its presence in countless biological structures and is of significant synthetic interest. Small-molecule amides are remarkable scaffolds for designing new drugs. Here, we report a new Ugi4CR approach using 5-amino-3,3-protected-oxindole derivatives, carboxylic acids (and nitrophenols), aldehydes (and ketones) and isocya...
N-Substituted 3-Aminooxindoles and N-Propargyl Derivatives: Potential Biologica...
Marques, Carolina; Carreiro, Elisabete; Hofmanova, Tereza; López, Óscar; T. García-Sosa, Alfonso; Leitzbach, Luisa; Stark, Holger; González-Bakker, AdayThe oxindole core is an important structural motif in many natural and synthetic substances with various biological activities including anticancer, antineurodegenerative, and antimicrobial properties. This report focuses on the synthesis and biological activity of a series of novel N-substituted 3-aminooxindoles and their assessment in cholinesterase (ChE) and monoamine oxidase (MAO) inhibition. With regard to...
N-Substituted 3-Aminooxindoles and N-Propargyl Derivatives: Potential Biologica...
Hofmanova, Tereza; Marques, Carolina; García-Sosa, Alfonso T.; López, Óscar; Leitzbach, Luisa; Carreiro, Elisabete P.; González-Bakker, AdayMCIN/AEI/10.13039/501100011033; PID2021-123059OB-I00 and PID2020-116460RB-I00
Tryptanthrin and Its Derivatives in Drug Discovery: Synthetic Insights
Brandão, Pedro; Pineiro, Marta; Burke, Anthony J.Tryptanthrin is a golden-yellow, naturally occurring alkaloid that can be obtained from multiple sources and through different synthetic methodologies. This tetracyclic compound displays several relevant biological activities. The potential of this tetracyclic alkaloid has been widely explored, and several researchers have focused their attention on expanding the variety of tryptanthrin derivatives by using a r...
N-1,2,3-triazole-isatin derivatives for cholinesterase and β-amyloid aggregatio...
Marques, Carolina S.; López, Óscar; Bagetta, Donatella; Carreiro, Elisabete P.; Petralla, Sabrina; Bartolini, Manuela; Hoffmann, MatthiasOur goal was the evaluation of a series of N-1,2,3-triazole-isatin derivatives for multi-target activity which included cholinesterase (ChE) inhibition and β-amyloid (Aβ) peptide anti-aggregation. The compounds have shown considerable promise as butyrylcholinesterase (BuChE) inhibitors. Although the inhibition of eel acet- ylcholinesterase (eeAChE) was weak, the inhibitions against equine BuChE (eqBuChE) and hu...
Accessing New 5-α-(3,3-Disubstituted Oxindole)-Benzylamine Derivatives from Isa...
Marques, Carolina Silva; McArdle, Patrick; Erxleben, Andrea; Burke, Anthony J.A one-step, three-component Petasis reaction of isatin derived 5-arylboronate-3-substituted oxindole derivatives with salicylaldehydes and secondary amines affords new enan- tiomerically pure structurally diverse 5-α-(3-substituted-oxind- ole)-benzylamine derivatives. The reaction shows good sub- strate and reagent scope affording the products with good to excellent yields (up to >99 % yield) and enantioselecti...
Ambipolar Pentacyclic Diamides with Interesting Electrochemical and Optoelectro...
Marques, Carolina S.; Cruz, Hugo; Lawrence, Simon E.; Gago, Sandra; Ramalho, João P. Prates; Morgado, Jorge; Branco, Luís C.; Burke, Anthony J.Developing organic semiconductors (OSCs) for organic thin film transistors (OTFT) and optoelectronic applications is a challenge. We developed highly crystalline pentacyclic diamides (3) and (4) which showed good OTFT and OLED potential and energy gaps of 2.60 eV and 2.54 eV. They exhibited interesting photo and eletroluminescence activity. Both compounds showed good quantum yields (0.56 for (3) and 0.6 for (4)).