Background: Coumarins are naturally occurring biologically active heterocyclic molecules endowed with a wide range of biological properties, including antibacterial, antifungal, and antitumor activities.

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.

背景：香豆素是天然存在的生物活性杂环分子，具有广泛的生物特性，包括抗菌、抗真菌和抗肿瘤活性。

目的：本工作旨在合成新的含香豆素化合物并研究其细胞毒活性。

方法：以三氟乙醇为溶剂，在50°C下，用合适的芳香胺和肽处理含环氧化物的香豆素衍生物，制备香豆素肽和香豆素氨基醇。评估了这些衍生物对三种不同细胞系的细胞毒活性：HeLa、MDA-MB-231 和 L-132。通过MTT（3-(4,5-二甲基噻唑-2-基)-2,5-二苯基溴化四唑）测定确定细胞活力。

结果：开发了一种用于合成 13 种新型香豆素肽和香豆素氨基醇衍生物的新方案。在测试的化合物中，三种衍生物对所有测试的细胞系都显示出显着的活性。对接研究表明，双取代的肽香豆素衍生物与人类雌激素受体活性位点的 Asp 351 和 Thr 347 氨基酸有良好的相互作用。

结论：结果表明合成的化合物可能是新型抗肿瘤化合物研究的有希望的候选物。