13 documents found, page 1 of 2
New (Iso)quinolinyl-pyridine-2,6-dicarboxamide G-Quadruplex Stabilizers. A Stru...
Cadoni, Enrico; Magalhães, Pedro R.; Emídio, Rita M.; Mendes, Maria Eduarda; Vítor, Jorge M. B.; Carvalho, Josué; Cruz, Carla; Victor, Bruno L.G-quadruplex (G4)-interactive small molecules have a wide range of potential applications, not only as drugs, but also as sensors of quadruplex structures. The purpose of this work is the synthesis of analogues of the bis-methylquinolinium-pyridine-2,6-dicarboxamide G4 ligand 360A, to identify relevant structure–activity relationships to apply to the design of other G4-interactive small molecules bearing bis-qu...
Comparative in vitro and in vivo antimalarial activity of the indole alkaloids ...
Silva, Luiz Francisco Rocha e; Montoia, Andréia; Amorim, Rodrigo C.N.; Melo, Márcia R.S.; Henrique, Marycleuma Campos; Nunomura, Sergio MassayoshiIndole alkaloids ellipticine (1), cryptolepine triflate (2a), rationally designed 11-(4-piperidinamino)cryptolepine hydrogen dichloride (2b) and olivacine (3) (an isomer of 1) were evaluated in vitro against Plasmodium falciparum and in vivo in Plasmodium berghei-infected mice. 1-3 inhibited P. falciparum (IC50 ≤ 1.4 μM, order of activity: 2b > 1 > 2a > 3). In vitro toxicity to murine macrophages was evaluated ...
Stereoselective Synthesis of Spirooxindole Derivatives Using One-Pot Multicompo...
Ghosh, Rajat; Vítor, Jorge M. B.; Mendes, Maria Eduarda; Paulo, Alexandra; Acharya, Pratap ChandraA highly stereoselective, one-pot, multicomponent method has been developed to synthesize pyrrolizidine- and N-methyl pyrrolidine-substituted spirooxindole derivatives. The [3 + 2] cycloaddition reaction involves the reaction between the dipole azomethine ylides, generated in situ from the reaction between isatin and secondary amino acids such as L-proline or sarcosine, and α,β-unsaturated carbonyl compounds as...
Combining 1,3-ditriazolyl-benzene and quinoline to discover a new G-quadruplex ...
Mendes, Maria Eduarda; Cadoni, Enrico; Carneiro, Filipa; Afonso, Marta; Brito, Hugo; Lavrado, João; Santos, Daniel J. V. A. dos; Vítor, Jorge M. B.Quadruplex nucleic acids are promising targets for cancer therapy. In this study we used a fragment-based approach to create new flexible G-quadruplex (G4) DNA-interactive small molecules with good calculated oral drug-like properties, based on quinoline and triazole heterocycles. G4 melting temperature and polymerase chain reaction (PCR)-stop assays showed that two of these compounds are selective G4 ligands, ...
The opposing effects of the flavonoids isoquercitrin and sissotrin, isolated fr...
Paulo, Alexandra; Martins, Sofia; Branco, Pedro; Dias, Teresa; Borges, Carlos; Rodrigues, Ana Isabel; Costa, Maria do Ceu; Teixeira, AdrianoThe effect of an aqueous extract of Pterospartum tridentatum on the blood glucose levels of normal Wistar rats was investigated in a situation of oral glucose challenge. The extract at 300 mg/kg showed an anti-hyperglycaemic effect in the first 30 min aft
Cryptolepine analogues containing basic aminoalkyl side-chains at C-11
Lavrado, Joao; Paulo, Alexandra; Gut, Jiri; Rosenthal, Philip J.; Moreira, RuiA series of cryptolepine derivatives has been synthesized through the incorporation of short basic side-chains in the C-11 position of the 10H-indolo[3,2-b] quinoline scaffold. Their antiplasmodial activity was evaluated in vitro against the chloroquine resistant Plasmodium falciparum W2 strain, showing IC50 values between 22 and 184 nM, while their cytotoxicity was assessed using HUVEC cells, revealing three c...
A new delta-7,22-sterol from the bulbs of Autonoë madeirensis
Paulo, Alexandra; Dias, Catarina; Jimeno, M. Luísa; Borges, Carlos; Nascimento, JoséThe spectral data of a new delta-7,22 sterol, 24S-ethyl-5-alfa-cholesta-7,22E-dien-3-alfa-O-beta-galactopyranoside, isolated from the bulbs of Autonoë madeirensis, are reported
Structural elucidation of natural 2-hydroxy di- and tricarboxylic acids and est...
Dias, Catarina; Dias, Mário; Borges, Carlos; Almoster Ferreira, M. A.; Paulo, Alexandra; Nascimento, JoséThe chemical composition of Autonoë madeirensis bulbs was characterized as part of a systematic phytochemical study of this species. The compounds reported were mainly identified on the basis of gas-chromatographic/electron ionization, electrospray ionization and tandem mass spectrometry. The structures of the pure compounds were also characterized by means of other physical and spectroscopic data (m.p., IR, UV...
Structural elucidation of natural 2-hydroxy di- and tricarboxilic acids and est...
Dias, Catarina; Dias, Mário; Borges, Carlos; Ferreira, M. A. Almoster; Paulo, Alexandra; Nascimento, JoséAutonoë madeirensis (Menezes) Speta is a Hyacinthaceae endemic from the Portuguese Archipelago of Madeira.1,2 Previous studies on Hyacinthaceae species have shown that they produce a large number of biologically important secondary metabolites, such as triterpenoid and steroid glycosides3, flavone and homoisoflavanone glycosides4 and polyhydroxyalkaloids.5 Included in a systematic phytochemical study of the bul...
Estudo Fitoquímico dos bolsos de Autonoë Madeirensis
Dias, Catarina; Dias, Mário; Jimeno, M. Luísa; Borges, Carlos; Nascimento, José; Paulo, AlexandraAutonoë madeirensis (Menezes) Speta, (Scilla maderensis Menezes), é uma Hyacinthaceae endémica do arquipélago da Madeira sobre a qual, até finais dos anos oitenta, era desconhecida qualquer investigação de natureza fitoquímica, farmacológica ou toxicológica. Por se tratar de uma espécie da flora nacional e porque estudos preliminares demonstraram que os seus bolbos possuíam substâncias com actividade farmacológ...