6 documents found, page 1 of 1
Preclinical validation of a new hybrid molecule loaded in liposomes for melanom...
Pinho, Jacinta O.; Matias, Mariana; Marques, Vanda; Eleutério, Carla; Fernandes, Célia; Gano, Lurdes; Amaral, Joana D.; Mendes, EduardaThe aggressiveness of melanoma and lack of effective therapies incite the discovery of novel strategies. Recently, a new dual acting hybrid molecule (HM), combining a triazene and a ʟ-tyrosine analogue, was synthesized. HM was designed to specifically be activated by tyrosinase, the enzyme involved in melanin biosynthesis and overexpressed in melanoma. HM displayed remarkable superior antiproliferative activity...
Fighting S. aureus catheter-related infections with sophorolipids: Electing an ...
Mendes, Rita M.; Francisco, Ana Paula; Carvalho, Filomena A.; Dardouri, Maïssa; Costa, Bruna; Bettencourt, Ana; Costa, Judite; Gonçalves, LídiaStaphylococcus aureus medical devices related-infections, such as blood stream catheter are of major concern. Their prevention is compulsory and strategies, not prone to the development of resistance, to prevent S. aureus biofilms on catheter surfaces (e.g. silicone) are needed. In this work two different approaches using sophorolipids were studied to prevent S. aureus biofilm formation on medical grade silicon...
A single-step multicomponent synthesis of a quinoline derivative and the charac...
Pinto, Luciana Matos Alves; Adeoye, Oluwatomide; Thomasi, Sérgio Scherrer; Francisco, Ana Paula; Marques, Helena CabralMulticomponent synthesis are convergent reactions in which three or more starting materials react in a single step to form the product. In the discovery and development of new drugs, multicomponent reactions offer several advantages over traditional synthesis: shorter experiment time, less need for laboratory techniques and scalability. Thus, the objective of this work was to perform the multicomponent synthesi...
Pyromellitic dianhydride crosslinked soluble cyclodextrin polymers: Synthesis, ...
Adeoye, Oluwatomide; Bártolo, Inês; Conceição, Jaime; Bento-Silva, Andreia; Duarte, Noélia; Francisco, Ana Paula; Taveira, Nuno; Marques, Helena CabralWe report the synthesis of water soluble cyclodextrin (CD) polymers prepared by crosslinking pyromellitic dianhydride (PMDA) with two CD derivatives (methyl-β-CD - MβCD and (2-hydroxy)propyl-β-CD - HPβCD) and their evaluation as functional sub-micron sized carriers in the development of antiretroviral drug delivery systems. Using the protease inhibitor lopinavir (LPV) as model drug, LPV loaded CD polymers (pHPβ...
Antimycobacterial metabolites from Plectranthus. Royleanone derivatives against...
Rijo, Patrícia; Simões, Maria de Fátima; Francisco, Ana Paula; Rojas, Rosário; Gilman, Robert H.; Vaisberg, Abraham J.; Rodríguez, BenjamínThe antimycobacterial activities of eight diterpenes, 1–8, isolated previously from Plectranthus and eleven esters, 9–19, of 7α-acetoxy-6β,12-dihydroxyabieta-8,12-diene-11,14-dione (5) were evaluated against the MTB strains H37Rv and MDR. Only diterpenoids with a quinone framework revealed anti-MTB activity. Abietane 5 and its 6,12-dibenzoyl, 12-methoxybenzoyl, 12-chlorobenzoyl, and 12-nitrobenzoyl esters, 9, 1...
Dopamine- and tyramine-based derivatives of triazenes
Perry, M. Jesus; Mendes, Eduarda; Simplicio, Ana Luisa; Coelho, Ana; Soares, Ricardo V.; Iley, Jim; Moreira, Rui; Francisco, Ana PaulaA range of triazene derivatives were synthesized and investigated as prodrug candidates for melanocyte-directed enzyme prodrug therapy (MDEPT). The prodrugs contained a tyramine or dopamine promoiety required for tyrosinase activation and this was joined via a urea functional group to the cytotoxic triazene. The stability of each of the prodrugs in phosphate buffer, human plasma and in mushroom tyrosinase is di...