Jump to main content
Jump to site search

Issue 35, 2017
Previous Article Next Article

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

Author affiliations

Abstract

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).

Graphical abstract: Synthesis and evaluation of selenium-containing indole chalcone and diarylketone derivatives as tubulin polymerization inhibition agents

Back to tab navigation

Supplementary files

Publication details

The article was received on 06 Jul 2017, accepted on 17 Aug 2017 and first published on 17 Aug 2017


Article type: Paper
DOI: 10.1039/C7OB01655G
Org. Biomol. Chem., 2017,15, 7404-7410

  •   Request permissions

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

    S. Zhang, B. An, J. Li, J. Hu, L. Huang, X. Li and A. S. C. Chan, Org. Biomol. Chem., 2017, 15, 7404
    DOI: 10.1039/C7OB01655G

Search articles by author

Spotlight

Advertisements