Background: Apoptosis is a route of cell death induced by a highly regulated intracellular program.
An increase in apoptotic activity could lead to neurodegenerative pathologies, whereas a decrease in apoptotic
activity could lead to uncontrolled cellular proliferation.
Objective: The aim of this research was to synthesize ten styrylheterocycle compounds, analogs of resveratrol,
having a thiophene ring substituted in position 2- or 3- and a benzene ring with one or two hydroxy and methoxy
groups. The compounds were evaluated for their cytotoxicity and apoptotic activity against the U-937 cancer cell
Method: The experiments were conducted at 1000 μM, 250 μM, 100 μM, and 50 μM in order to measure apoptotic
activity (% hypodiploid nuclei). The cytotoxicity was expressed as the concentration of a substance able to
inhibit 50% of the metabolic activity in an MTS assay (maCC50), and as the percentage of cellular death (% Death
Cell.) at 1000 μM and 100 μM.
Results: Changing the phenyl group in a thienyl group occupying the 2- or 3-position almost always leads to an
improvement in apoptosis. In addition, whereas the presence of a hydroxy group makes the molecules more cytotoxic
than resveratrol, it also improves apoptosis. However, the presence of a methoxy group in the phenyl ring
leads to collapse of the cytotoxicity, thereby allowing an increase in the analytical concentrations, and verifying
that, at 1000 μM, the compounds 3b and 3c show apoptosis levels of 81% and 72%, respectively.
Conclusion: We look forward to synthesizing other heterocyclic molecules to find even more active derivatives
endowed with anti-cancer potential.