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Antioxidant, Antitumor and Bactericidal Activities of Ethyl Gallate Quinoxalines



Quinoxaline, a fused heterocycle of benzene and pyrazine rings are becoming
recognized as a potent class of anti-cancer compounds, such as, in a wide array of pharmacological
activities.



We evaluate the three gallate quinoxalines (G-A1, G-A2, and G-A3) as c-Met kinase inhibitors
using a docking study, in vitro anticancer potential measurements, antioxidant and bactericidal activities.



The docking study showed hydrogen bond linkage of quinoxalines with amino acids at active
site of c-Met kinase structures, indicating a possible cancer inhibition cell proliferation. Therefore, the
three quinoxalines were analyzed against four in vitro cancer cell lines, and G-A1 demonstrated cytotoxicity
against HL-60 and HCT116 cell lines (IC50= 9.55 and IC50= 16.67 μmol L-1, respectively). In
HepG2 and MCF-7 cells, the IC50 were 22.48 and 33.42 μmol L-1, respectively. For G-A2 and G-A3,
cytotoxic activity ranged from 61.22 to >101.21 μmol L-1. Potent antioxidant activities were also obtained
for G-A2>G-A1>G-A3 (IC50= 4.5-8.4 μmol L-1 and AAI= 8.8-17.8). Six different Bacillius
strains showed growth inhibition (11.33 to 13.33 mm) in the presence of quinoxaline G-A1 (500 μg).



The present work showed the biological potential of quinoxalines G-A1, G-A2 and G-A3
in inhibiting four cancer cells proliferation, in addition to a very strong antioxidant activity.
