Síntese de derivados quinolínicos, 1,2,3-triazóis e análogos do resveratrol: avaliação antitumoral e antiparasitária

Abstract

In this study, 32 compounds were synthesized, 21 of which are novel. These compounds were biologically evaluated on L. amazonensis, P. Falciparum strains and MDA-MB-231 tumor cells, based on their structural profiles. The rationalization and synthetic strategy to obtain heterocyclic compounds and their salts were guided by molecular hybridization and insertion of functional groups. Compounds from three different classes were synthesized: 1,2,3-triazoles, 1,4-disubstituted by aliphatic chains and their salts; quinoline derivatives; and resveratrol analogues. In the biological evaluations, the multitarget action of the Q4 derivative and the antitumor activity of TS4 stood out. For the antimalarial evaluation, Q4 presented an IC50 of 0.44 ± 3.98 μM and an IS >226.15 against the P. falciparum strain, being superior to the positive control. Furthermore, for the antileishmanial evaluation, Q4 presented an IC50 of 22.35 ± 1.97 μM and an IS >6.71 against the amastigote form of L. amazonensis. The TS4 derivative exhibited a low IC50 value of 5.6 μM against MDAMB-231 tumor cells, in addition to the ability to prevent the clonogenic survival of new colonies of MDA-MB-231 tumor cells.