期刊
MOLECULES
卷 26, 期 4, 页码 -出版社
MDPI
DOI: 10.3390/molecules26040786
关键词
coumarin sulfonamides; coumarin amides; MDA-MB-231; antitumor
资金
- Natural Science Foundation of Guangdong Province [2018A0303130139, 2017A030310488]
- Science and Technology Planning Project of Guangdong Province [2015A020211039]
- Scientific Research Project for Guangzhou Municipal Colleges and Universities [1201610139, 1201630263]
- Science and Technology Program of Guangzhou [201707010353]
- Educational Commission of Guangdong Province [2015KQNCX134]
Coumarin derivatives have good antitumor activity, with compound 9c showing strong antitumor effects in MDA-MB-231 cells, indicating potential for further research.
Coumarins possesses immeasurable antitumor potential with minimum side effects depending on the substitutions on the basic nucleus, which exhibits great prospects for antitumor drug development. In an attempt to develop novel antitumor candidates, a series of coumarin sulfonamides and amides derivatives were designed and synthetized. The majority of these derivatives showed good cytotoxic activity against MDA-MB-231 and KB cell lines, among which compound 9c was the most potent against MDA-MB-231 cells, with IC50 value of 9.33 mu M, comparable to 5-fluorouracil. Further investigation revealed that compound 9c had versatile properties against tumors, including inhibition of cell migration and invasion as well as inducing apoptosis. Reactive oxygen species (ROS) assay and western blotting analysis suggested that compound 9c promoted cancer cell apoptosis by increasing ROS levels and upregulating the expression of caspase-3 in MDA-MB-231 cells. These results indicated that compound 9c could be promising lead compound for further antitumor drug research.
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