Coumarin Sulfonamides and Amides Derivatives: Design,Synthesis, and Antitumor Activity In Vitro |
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| Authors: | Jing Zhang Yaling Tan Guorong Li Lexian Chen Minyi Nie Zhaohua Wang Hong Ji |
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| Institution: | 1.Key Laboratory of Molecular Target & Clinical Pharmacology and the State Key Laboratory of Respiratory Disease, School of Pharmaceutical Sciences & the Fifth Affiliated Hospital, Guangzhou Medical University, Guangzhou 511436, China; (J.Z.); (Y.T.); (G.L.); (L.C.); (M.N.);2.School of Basic Medical Sciences, Guangzhou Medical University, Guangzhou 511436, China; |
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| Abstract: | 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 μM, 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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| Keywords: | coumarin sulfonamides coumarin amides MDA-MB-231 antitumor |
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