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The design, synthesis and evaluation of selenium-containing 4-anilinoquinazoline hybrids as anticancer agents and a study of their mechanism

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Abstract

Inhibition of tubulin polymerization is one of the significant strategies in the treatment of cancer. Inspired by the excellent antitumor activity of EP128495 and the beneficial biological activities of selenium compounds, a series of new selenium-containing 4-anilinoquinazoline hybrids were synthesized and evaluated as tubulin polymerization inhibitors. An anti-proliferative activity assay showed that most of the compounds inhibited human sensitive cancer cells at low nanomolar concentrations. A mechanism study revealed that the optimal compound 5a disrupted microtubule dynamics, decreased the mitochondrial membrane potential and arrested HeLa cells in the G2/M phase, finally resulting in cellular apoptosis.

Graphical abstract: The design, synthesis and evaluation of selenium-containing 4-anilinoquinazoline hybrids as anticancer agents and a study of their mechanism

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Publication details

The article was received on 17 Apr 2018, accepted on 30 May 2018 and first published on 31 May 2018


Article type: Paper
DOI: 10.1039/C8OB00875B
Citation: Org. Biomol. Chem., 2018, Advance Article
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    The design, synthesis and evaluation of selenium-containing 4-anilinoquinazoline hybrids as anticancer agents and a study of their mechanism

    B. An, S. Zhang, J. Hu, T. Pan, L. Huang, J. C. Tang, X. Li and A. S. C. Chan, Org. Biomol. Chem., 2018, Advance Article , DOI: 10.1039/C8OB00875B

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