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Synthesis and evaluation of selenium-containing indole chalcone and diarylketone derivatives as tubulin polymerization inhibition agents. 2017

Shun Zhang, and Baijiao An, and Jiayan Li, and Jinhui Hu, and Ling Huang, and Xingshu Li, and Albert S C Chan
School of Pharmaceutical Sciences, Sun Yat-sen University, Guangzhou 510006, China. huangl72@mail.sysu.edu.cn lixsh@mail.sysu.edu.cn.

Sixteen new selenium-containing indole chalcone and diarylketone derivatives were synthesized and evaluated as tubulin polymerization inhibitors. Among them, compound 25b exhibited the most potent antiproliferative activities against six human cancer cell lines with IC50 values of 0.004-0.022 μM. A microtubule dynamics assay and an immunofluorescence assay confirmed that 25b could effectively inhibit tubulin polymerization (IC50 = 2.1 ± 0.27 μM). Further cellular mechanism studies revealed that 25b induced G2/M phase arrest, which was further evidenced by the decrease in the mitochondrial membrane potential (MMP).

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