165 documents found, page 1 of 17
Development of eugenol derivatives with 5-LOX inhibitory activity
Filho, José L. Pereira; Pereira, Renato B.; Vieira, Tatiana F.; Sousa, Sérgio F.; Coelho, José Ricardo Alves; Pinto, Nuno F. S.; Coelho, Catarina M. M.Eugenol (4-allyl-2-methoxyphenol), is the major chemical constituent in the essential oil of numerous plant species. Several biological properties have been described for this molecule, including modulation of enzymatic targets relevant for the inflammatory response, such as 5-lipoxygenase (5-LOX). As so, there is interest in expanding the chemical space of this molecule to develop new molecules to be used in i...
New cation sensors based on eugenol-derived azo dyes
Coelho, José R. A.; Pacheco, Ana Rita Faria; Domingues, Diogo C.; Rodrigues, Ana Rita Oliveira; Temitope, Akani A.; Coutinho, Paulo J. G.Eugenol-based azo dyes illustrate how bio-sourced compounds like eugenol can be transformed through synthetic processes into functional and colorful compounds. The main purpose of the present work was to develop new responsive colorimetric sensors for metal cations based on eugenol-derived azo compounds. The incorporation of the azo group into the eugenol framework allows for strong electronic interactions with...
Benzo[a]phenoxazines as potential anti-inflammatory drugs
Pinto, Joana; Gonçalves, M. Sameiro T.; Pereira, David M.The chemical diversity of natural products provides a promising source of anti-inflammatory drugs, notably targeting COX-2, whose activity is associated with inflammatory processes and carcinogenesis. The COX-2 and LOX inhibitory capacity of several benzo[a]phenoxazines, N- and O-heterocyclic compounds, was studied. The kinetic assay results revealed that these molecules significantly inhibit COX-2 activity, hi...
Synthesis, photophysics, and potential antifungal activity of Benzo[a]phenoxazines
Guimarães, Bárbara S. G.; Sousa, Maria João; Gonçalves, M. Sameiro T.The synthesis and full characterization of new hydroxyl benzo[a]phenoxazinium chlorides with N-(di)propyl and/or N-isopropyl groups in the 5 and 9 positions are described. Photophysical studies carried out in ethanol and water revealed strong absorbances and significant fluorescence emissions at up to 676 nm. The antifungal activity was assessed against Saccharomyces cerevisiae and the results provide possible ...
Anticancer activity of benzo[a]phenoxazine compounds promoting lysosomal dysfun...
Ferreira, João Carlos Canossa; Gonçalves, M. Sameiro T.; Preto, Ana; Sousa, Maria JoãoSpecific cancer therapy remains a problem to be solved. Breast and colorectal cancer are among the cancers with the highest prevalence and mortality rates. Although there are some therapeutic options, there are still few effective agents for those cancers, which constitutes a clinical problem that requires further research efforts. Lysosomes play an important role in cancer cells’ survival, and targeting lysoso...
Combining fluconazole with benzo[a]phenoxazine derivatives as a promising strat...
Pacheco, Maria Inês Costa; Guimarães, Bárbara; Pereira-Silva, Patrícia; Costa-Barbosa, Augusto; Gonçalves, M. Sameiro T.; Sousa, Maria JoãoThe rise in non-albicans Candida species, exhibiting unpredictable antifungal resistance, complicates treatment and contributes to the growing threat of invasive, life-threatening infections. This study evaluates the antifungal activity of four benzo[a]phenoxazine derivatives (C34, C35, A42, and A44) against 14 Candida strains following EUCAST standards. Fluconazole interactions are analysed through fractional ...
Targeting lysosomes in colorectal cancer: exploring the anticancer activity of ...
Ferreira, João C. C.; Granja, Sara; Almeida, Ana F.; Baltazar, Fátima; Gonçalves, M. Sameiro T.; Preto, Ana; Sousa, Maria JoãoColorectal cancer (CRC) has been ranked as one of the cancer types with a higher incidence and one of the most mortal. There are limited therapies available for CRC, which urges the finding of intracellular targets and the discovery of new drugs for innovative therapeutic approaches. In addition to the limited number of effective anticancer agents approved for use in humans, CRC resistance and secondary effects...
Novel benzo[α]phenoxazinium chlorides functionalized with sulfonamide groups as...
Ferreira, J. C. C.; Sousa, Rui Pedro Carvalho Lima; Preto, Ana; Sousa, Maria João; Gonçalves, M. Sameiro T.The demand for new fluorophores for different biological target imaging is increasing. Benzo[<i>a</i>]phenoxazine derivatives are fluorochromophores that show promising optical properties for bioimaging, namely fluorescent emission at the NIR of the visible region, where biological samples have minimal fluorescence emission. In this study, six new benzo[<i>a</i>]phenoxazinium chlorides possessing sulfonamide gr...
Phenolic compounds contribution to portuguese propolis anti-melanoma activity
Caetano, Ana Rita; Oliveira, Rafaela Dias; Celeiro, Sónia Pires; Freitas, Ana Sofia; Cardoso, Susana M.; Gonçalves, M. Sameiro T.; Baltazar, FátimaMelanoma is the deadliest type of skin cancer, with about 61,000 deaths annually worldwide. Late diagnosis increases mortality rates due to melanoma’s capacity to metastasise rapidly and patients’ resistance to the available conventional therapies. Consequently, the interest in natural products as a strategy for drug discovery has been emerging. Propolis, a natural product produced by bees, has several biologic...
Targeting lysosomes in colorectal cancer: exploring the anticancer activity of ...
Ferreira, João C. C.; Granja, Sara Costa; Almeida, Ana F.; Baltazar, Fátima; Gonçalves, M. Sameiro T.; Preto, Ana; Sousa, Maria JoãoColorectal cancer (CRC) has been ranked as one of the cancer types with a higher incidence and one of the most mortal. There are limited therapies available for CRC, which urges the finding of intracellular targets and the discovery of new drugs for innovative therapeutic approaches. In addition to the limited number of effective anticancer agents approved for use in humans, CRC resistance and secondary effects...