Potencial citotóxico de derivados sintéticos de quinolinas em linhagem de adenocarcinoma colorretal humano

Abstract

Quinolines are heterocyclic nitrogen compounds consisting of a benzene ring fused to a pyrimidine. They are present in many natural substances, especially in plants alkaloids and synthetic compounds. Initially used as antimalarial drug, today present many other biological activities: tuberculosis, antibacterial, antifungal, antioxidant, antiinflammatory and antidepressant. Furthermore, many compounds that show quinoline rings in its structure have anticancer activity. This property is interesting for the development of new drugs to combat cancer. In this study, new derivatives of quinolines 1-(7-Chloroquinolin-4-yl)-5-methyl-Nphenyl-1H-1,2,3-triazole-4-carboxamide (QTCA1), 1-(7-Chloroquinolin-4-yl)-N-(4- fluorophenyl)-5-methyl-1H-1,2,3-triazole-4-carboxamide (QTCA4) and 7-chloro-4- (phenylselanyl)quinoline (QSPH) were evaluated for cytotoxic potential and ability to induce apoptosis in human colorectal adenocarcinoma cell line (HT-29). The compounds were tested alone and in combination with 5-fluorouracil (5-FU). QSPH showed potent cytotoxic effect inhibiting cell growth. Combinations of quinoline derivative QTCA4 with 5-FU enhanced drug cytotoxicity.