Background: Coumarins are naturally occurring biologically active heterocyclic molecules
endowed with a wide range of biological properties, including antibacterial, antifungal, and antitumor
Objective: The present work was aimed to synthesize new coumarin-containing compounds and to
investigate their cytotoxic activity.
Methods: Coumarin peptide and coumarin amino alcohols were prepared by treating epoxidecontaining
coumarin derivatives with suitable aromatic amines and peptides in trifluoroethanol as a
solvent at 50°C. These derivatives were evaluated for their cytotoxic activity on three different cell
lines: HeLa, MDA-MB-231 and L-132. Cell viability was determined by MTT (3-(4,5-
dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide) assay.
Results: A new protocol was developed for the synthesis of thirteen novel coumarin peptide and
coumarin amino alcohol derivatives. Among the tested compounds, three derivatives showed significant
activity against all the tested cell lines. Docking studies indicated favorable interactions of the
disubstituted peptide coumarin derivatives with the Asp 351 and Thr 347 amino acids at the active
site of the human estrogen receptor.
Conclusions: The results suggest that the synthesized compounds may be promising candidates in the
research of new antitumor compounds.