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Molecules 2015, 20(10), 18565-18584; doi:10.3390/molecules201018565

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

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
These authors contributed equally to this work.
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Author to whom correspondence should be addressed.
Academic Editor: Roman Dembinski
Received: 1 August 2015 / Revised: 3 October 2015 / Accepted: 7 October 2015 / Published: 13 October 2015
(This article belongs to the Section Bioorganic Chemistry)
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Abstract

In this study, two series of 3-oxo-3H-benzo[f]chromene-2-carboxylic acid derivatives (compounds 5ai and 6ag) 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. View Full-Text
Keywords: 3-oxo-3H-benzo[f]chromene-2-carboxylic acid derivatives; proliferation inhibitory activity; photophysical property; antitumor; biological imaging 3-oxo-3H-benzo[f]chromene-2-carboxylic acid derivatives; proliferation inhibitory activity; photophysical property; antitumor; biological imaging
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This is an open access article distributed under the Creative Commons Attribution License which permits unrestricted use, distribution, and reproduction in any medium, provided the original work is properly cited. (CC BY 4.0).

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MDPI and ACS Style

Fu, X.-B.; Wang, X.-F.; Chen, J.-N.; Wu, D.-W.; Li, T.; Shen, X.-C.; Qin, J.-K. Synthesis, Fluorescence Properties, and Antiproliferative Potential of Several 3-Oxo-3H-benzo[f]chromene-2-carboxylic Acid Derivatives. Molecules 2015, 20, 18565-18584.

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