| Summary: | 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 <b>9c</b> was the most potent against MDA-MB-231 cells, with IC<sub>50</sub> value of 9.33 μM, comparable to 5-fluorouracil. Further investigation revealed that compound <b>9c</b> 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 <b>9c</b> 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<b> 9c</b> could be promising lead compound for further antitumor drug research.
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