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Colon Adenocarcinoma Multidrug Resistance Reverted by Euphorbia Diterpenes: Structure-Activity Relationships and Pharmacophore Modeling

Colon Adenocarcinoma Multidrug Resistance Reverted by Euphorbia Diterpenes

Multidrug resistance (MDR) is a limiting step on the success of cancer chemotherapy. The drug efflux mediated by P-gp (P- glycoprotein) is one of the best studied mechanisms of MDR. This paper focuses on the inhibitory P-gp efflux activity, pharmacophore… Read more ›

Daniel J.V.A. dos Santos
Cancer, Multidrug resistance, P-gp/ABCB1
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Design, synthesis and structure–activity relationships of (1H-pyridin-4-ylidene)amines as potential antimalarials

structure–activity relationships (1H-pyridin-4-ylidene)amines antimalarials

(1H-Pyridin-4-ylidene)amines containing lipophilic side chains at the imine nitrogen atom were prepared as potential clopidol isosteres in the development of antimalarials. Their antiplasmodial activity was evaluated in vitro against the Plasmodium falciparum W2 (chloroquine-resistant) and FCR3 (atovaquone-resistant) strains. The most… Read more ›

Daniel J.V.A. dos Santos
Malaria
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