The synthesis and evaluation of new butadiene derivatives as tubulin polymerization inhibitors

Publication date: 15 June 2017
Source:Bioorganic & Medicinal Chemistry, Volume 25, Issue 12
Author(s): Yanqing Pang, Jun Yan, Baijiao An, Ling Huang, Xingshu Li
A series of new butadiene derivatives was synthesized and evaluated as tubulin polymerization inhibitors for the treatment of cancer. The optimal butadiene derivative, 9a, exhibited IC50 values of 0.056–0.089μM for five human cancer cell lines. This paper included a mechanistic study of the antiproliferative activity, including a tubulin polymerization assay, an examination of morphological alterations of cancer cells, an analysis of cell cycle arrest and an apoptosis assay.

Graphical abstract

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