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Synthesis Fluorescence Properties and Antiproliferative Potential of Several 3-Oxo-3H-benzofchromene-2-carboxylic Acid Derivatives

机译:几种3-Oxo-3H-苯并f亚甲基-2-羧酸衍生物的合成荧光性质和抗增殖潜力

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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.
机译:在这项研究中,两个系列的3-oxo-3H-苯并[f]亚甲基-2-羧酸衍生物(化合物> 5a – > i 和> 6a – > g )。评估了它们对A549和NCI-H460人非小细胞肺癌(NSCLC)细胞系的体外增殖抑制活性。测量了它们的光物理性质。在这些目标化合物中,> 5e 通过诱导细胞凋亡,阻止细胞周期和升高细胞内活性氧(ROS)水平表现出最强的抗增殖活性,表明它可能是有效的抗肿瘤药。此外,具有极低细胞毒性的化合物> 6g 具有出色的荧光特性,可作为生物成像的有效荧光探针。

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