12 documents found, page 1 of 2
Recent advances in fluorescent theranostics for Alzheimer's disease: a comprehe...
Francisco, Telmo N.; Malafaia, Daniela; Melo, Lúcia; Silva, Artur M. S.; Albuquerque, Hélio M. T.Alzheimer's disease (AD) is the most common form of neurodegenerative dementia that is rapidly becoming a major health problem, especially in developed countries because of their increasing life expectancy. Two main problems are often associated with the disease: (i) the absence of a widely accessible "gold-standard" for early diagnosis and (ii) lack of effective therapies with disease-modifying effects. The re...
Drug discovery based on oxygen and nitrogen (non-)heterocyclic compounds develo...
Sousa, Joana L. C.; Albuquerque, Hélio M. T.; Silva, Artur M. S.Artur Silva's research group has a long history in the field of medicinal chemistry. The development of new synthetic methods for oxygen (mostly polyphenols, e.g., 2- and 3-styrylchromones, xanthones, flavones) and nitrogen (e.g., pyrazoles, triazoles, acridones, 4-quinolones) heterocyclic compounds in order to be assessed as antioxidant, anti-inflammatory, antidiabetic, and anticancer agents has been the main ...
2,2’-[(1E,1’E)-{[Hexa-2,4-diyne-1,6-diylbis(oxy)]bis(2,1-phenylene)}bis(ethene-...
Malafaia, Daniela; Sousa, Joana L. C.; Silva, Artur M. S.; Albuquerque, Hélio M. T.2-Styrylchromones (2-SCs) are interesting compounds for their biological properties as well as versatility as starting materials for further transformations. Herein, we disclose a new 2-SC derivative—2,2’-[(1E,1’E)-{[hexa-2,4-diyne-1,6-diylbis(oxy)]bis(2,1-phenylene)}bis(ethene-2,1- diyl)]bis(4H-chromen-4-one)—which is a dimeric compound formed by two units of 2-SC linked through a 1,3-diyne moiety. It was obta...
6-[(2S,3R)-3-(2,4-Difluorophenyl)-3-hydroxy-4-(1H-1,2,4-triazol-1-yl)butan-2-yl...
Sousa, Joana L. C.; Albuquerque, Hélio M. T.; Silva, Artur M. S.Voriconazole (VN) is an antifungal drug indicated for the treatment of several fungal infections. Due to its side effects, some works involving late-stage functionalization of VN have been reported in the literature. Here, we disclose a new VN derivative, the 6-[(2S,3R)-3-(2,4-difluorophenyl)- 3-hydroxy-4-(1H-1,2,4-triazol-1-yl)butan-2-yl]-5-fluoropyrimidine-4-carbaldehyde (VNCHO). This compound results from th...
Gossypetin is a novel modulator of inflammatory cytokine production and a suppr...
Proença, Carina; Rufino, Ana Teresa; Santos, Isabela; Albuquerque, Hélio M. T.; Silva, Artur M. S.; Fernandes, EduardaOsteosarcoma (OS) is a common childhood sarcoma, and its treatment is hindered by adverse effects, chemoresistance, and recurrence. Interleukin (IL)-6 production by tumors plays a significant role in inflammation, carcinogenesis, and metastasis. This study aimed to investigate the antiproliferative potential of luteolin derivatives in OS and to evaluate interleukin production. MG-63, Saos-2, HOS, and 143B human...
Selective induction of DNA damage and cell cycle arrest mediated by chromone-tr...
Saher, Liza; Monteiro, Fátima L.; Rocha, Djenisa H. A.; Albuquerque, Hélio M. T.; Silva, Artur M. S.; Helguero, Luisa A.Chromones and triazoles are groups of heterocyclic compounds widely known to exhibit a broad spectrum of biological activities. The combination of these two pharmacophores could result in multiple mechanisms of action to increase the potency of anticancer drugs and reduce their side effects. The in vitro antitumor effect of eight chromone-based compounds was evaluated in breast (T-47D and MDA-MB-231) and prosta...
Microwave-assisted synthesis of 4,6-disubstituted isoindoline-1,3-diones by Die...
Nouali, Fatiha; Sousa, Joana L. C.; Albuquerque, Hélio M. T.; Mendes, Ricardo F.; Almeida Paz, Filipe A.; Saher, Liza; Kibou, ZahiraThe synthesis of 4,6-disubstituted isoindoline-1,3-diones through microwave-assisted Diels-Alder (DA) reactions is reported. Chromones bearing an α,β-unsaturated carbonyl system at C-3 were used as dienes and a scope of maleimides as dienophiles was investigated. The proposed mechanism involves a DA reaction of 3-benzoylvinylchromones with different maleimides, followed by chromanone ring opening and in situ ox...
Mild synthesis of symmetric 3,5-disubstituted nitrobenzenes
Francisco, Telmo N.; Sousa, Joana L. C.; Guieu, Samuel; Silva, Artur M. S.; Albuquerque, Hélio M. T.A mild synthesis of 3,5-disubstituted nitrobenzenes from readily available 3-formylchromones is reported. The developed methodology follows a cascade process, promoted by 1,8-diazabicyclo[5.4.0]undec-7-ene. The proposed mechanism involves an initial Michael addition of nitromethane at C-2 of a 3-formylchromone. The resultant intermediate undergoes another Michael reaction with a second 3-formylchromone molecule...
Steroid-quinoline hybrids for disruption and reversion of protein aggregation p...
Albuquerque, Hélio M. T.; Silva, Raquel Nunes da; Pereira, Marisa; Maia, André; Guieu, Samuel; Soares, Ana Raquel; Santos, Clementina M. M.Reversing protein aggregation within cells may be an important tool to fight protein-misfolding disorders such as Alzheimer's, Parkinson's, and cardiovascular diseases. Here we report the design and synthesis of a family of steroid-quinoline hybrid compounds based on the framework combination approach. This set of hybrid compounds effectively inhibited Aβ1-42 self-aggregation in vitro by delaying the exponentia...
Cholesterol chemistry and laboratory synthesis
Albuquerque, Hélio M. T.; Santos, Clementina M. M.; Silva, Artur M. S.Cholesterol (or cholest-5-en-3β-ol) is an essential component of cell membranes and also serves as the precursor for the synthesis of steroid hormones, bile acids, and vitamin D. Its total synthesis was one of the most remarkable achievements of 20th century Chemistry, accomplished almost simultaneously by Robinson in Oxford and Woodward at Harvard. This notable synthetic endeavor is on the basis of the followi...