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Repurposing antiplasmodial leads for cancer: Exploring the antiproliferative ef...

Fonte, Mélanie; Rôla, Catarina; Santana, Sofia; Ferraz, Ricardo; Prudêncio, Miguel; Almeida, Joana; Ferraz, Ricardo; Prudêncio, Cristina

Drug repurposing and rescuing have been widely explored as cost-effective approaches to expand the portfolio of chemotherapeutic agents. Based on the reported antitumor properties of both trans-cinnamic acids and quinacrine, an antimalarial aminoacridine, we explored the antiproliferative properties of two series of N-cinnamoyl-aminoacridines recently identified as multi-stage antiplasmodial leads. The compound...


Design, synthesis and antiplasmodial evaluation of new amide-, carbamate-, and ...

Marinović, Marina; Rimac, Hrvoje; de Carvalho, Lais Pessanha; Rôla, Catarina; Santana, Sofia; Pavić, Kristina; Held, Jana; Prudêncio, Miguel

Malaria, one of the oldest parasitic diseases, remains a global health threat, and the increasing resistance of the malaria parasite to current antimalarials is forcing the discovery of new, effective drugs. Harmicines, hybrid compounds in which harmine/β-carboline alkaloids and cinnamic acid derivatives are linked via an amide bond or a triazole ring, represent new antiplasmodial agents. In this work, we used ...


The effect of dosage on the protective efficacy of whole-sporozoite formulation...

Moita, Diana; Rôla, Catarina; Nunes-Cabaço, Helena; Nogueira, Gonçalo; Maia, Teresa G.; Othman, Ahmad Syibli; Franke-Fayard, Blandine; Janse, Chris J.

Immunization with Plasmodium sporozoites, either attenuated or administered under the cover of an antimalarial drug, can induce strong protection against malaria in pre-clinical murine models, as well as in human trials. Previous studies have suggested that whole-sporozoite (WSpz) formulations based on parasites with longer liver stage development induce higher protection, but a comparative analysis of four dif...


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