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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 ...
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, ...