The synthesis and evaluation of new butadiene derivatives as tubulin polymerization inhibitors. Issue 12 (15th June 2017)

• Record Type: Journal Article
• Authors: Pang, Yanqing; Yan, Jun; An, Baijiao; Huang, Ling; Li, Xingshu
• Is Part Of: Bioorganic & medicinal chemistry. Volume 25:Issue 12(2017)
• Page Start: 3059
• Page End: 3067
• Publication Date: 2017-06-15
• Subjects: CA-4 combretastatin A-4 -- MTT 3-(4, 5-dimethyl-2-thiazolyl)-2, 5-diphenyl-2-H-tetrazolium bromide -- PI propidium iodide -- FBS foetal bovine serum -- RH relative humidity -- TLC layer chromatography -- HPLC high-performance liquid chromatography -- DAPI 4′, 6-diamidino-2-phenylindole -- PBS phosphate-buffered solution; Butadiene derivatives -- Tubulin polymerization inhibitors -- Antiproliferative -- Cell cycle arrest -- Apoptosis -- Morphological alterations; Bioorganic chemistry -- Periodicals; Pharmaceutical chemistry -- Periodicals; Biochemistry -- Periodicals; Chemistry, Clinical -- Periodicals; Chemistry, Organic -- Periodicals; Chimie bio-organique -- Périodiques; Chimie pharmaceutique -- Périodiques; 615.19
• DOI: 10.1016/j.bmc.2017.03.066
• Languages: English
• ISSNs: 0968-0896

Abstract

Graphical abstract: Abstract: 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 0.056–0.089 μM 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.