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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, Eduarda

The 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...


Enantiopure Indolizinoindolones with in vitro activity against blood- and liver...

Pereira, Nuno A. L.; Monteiro, Ângelo; Machado, Marta; Gut, Jiri; Molins, Elies; Perry, Maria Jesus; Dourado, Jorge; Moreira, Rui; Rosenthal, Philip J.

Malaria continues to be a major cause of morbidity and mortality to this day, and resistance to drugs like chloroquine has led to an urgent need to discover novel chemical entities aimed at new targets. Here, we report the discovery of a novel class of potential antimalarial compounds containing an indolizinoindolone scaffold. These novel enantiopure indolizinoindolones were synthesized, in good-to-excellent yi...


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