Synthesis, Fluorescence Properties, and Antiproliferative Potential of Several 3-Oxo-3H-benzo[f]chromene-2-carboxylic Acid Derivatives

Molecules

Xian-Fu Wang¹  Xiao-Bo Fu¹  Xing-Can Shen¹  Ting Li¹  Jia-Nian Chen¹  De-Wen Wu¹  Jiang-Ke Qin¹ 

[1] State Key Laboratory Cultivation Base for the Chemistry and Molecular Engineering of Medicinal Resources, School of Chemistry & Pharmacy, Guangxi Normal University, Yucai Road 15,Guilin 541004, China;

关键词: 3-oxo-3H-benzo[f]chromene-2-carboxylic acid derivatives;    proliferation inhibitory activity;    photophysical property;    antitumor;    biological imaging;   

DOI  :  10.3390/molecules201018565

来源: DOAJ

【 摘 要 】

In this study, two series of 3-oxo-3H-benzo[f]chromene-2-carboxylic acid derivatives (compounds 5a–i and 6a–g) were synthesized. Their in vitro proliferation inhibitory activities against the A549 and NCI-H460 human non-small cell lung cancer (NSCLC) cell lines were evaluated. Their photophysical properties were measured. Among these target compounds, 5e exhibited the strongest antiproliferative activity by inducing apoptosis, arresting cell cycle, and elevating intracellular reactive oxygen species (ROS) level, suggesting that it may be a potent antitumor agent. In addition, compound 6g with very low cytotoxicity, demonstrated excellent fluorescence properties, which could be used as an effective fluorescence probe for biological imaging.

【 授权许可】

Unknown