化学
查尔酮
细胞毒性
阿霉素
癌细胞
立体化学
组合化学
产量(工程)
羟醛反应
IC50型
细胞培养
生物化学
体外
癌症
化疗
内科学
材料科学
冶金
催化作用
外科
生物
医学
遗传学
作者
Olívia Pontes,Marta Costa,Filipa Santos,Belém Sampaio‐Marques,Tatiana A. Dias,Paula Ludovico,Fátima Baltazar,M. Fernanda Proença
标识
DOI:10.1016/j.ejmech.2018.07.058
摘要
Chalcone and chromene derivatives were synthesized in good yield through simple and effective reactions using innocuous solvents such as water and ethanol and high yielding aldol condensations. Generally, the reactions were performed at room temperature, leading to the isolation of highly pure compounds. These compounds were tested on breast cancer cells (MCF-7 and Hs578T) and breast non-neoplastic cells (MCF-10A). After determination of IC50 value, specific assays were performed to analyze the potential of these compounds, and those bearing halogenated substituents presented enhanced activity comparing to methoxyl or methyl groups. More specifically, the bromine atom was often present in the bioactive molecules that proceeded to the final assays and showed to be promising candidates for further studies. The selected chromene acted as a cell migration inhibitory agent and triggered regulated cell death associated with G2/M cell-arrest and microtubule destabilization. For chalcones, the results suggest an anti-proliferative activity. Also, results for combination-therapy potentiated the antitumor effect of doxorubicin and reduced cytotoxicity in MCF-10A cells.
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