Design, synthesis and biological evaluation of 3,4-diaryl-1,2,5-oxadiazole-2/5-oxides as highly potent inhibitors of tubulin polymerization.

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ID: 4709
2019
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Abstract
Structure-activity relationships for rigid analogues of combretastatin A-4 (CA-4) were investigated, leading to the discovery of a series of 3,4-diaryl-1,2,5-oxadiazole-N-oxides. Among them, 7n' and 7n'' showed remarkable antiproliferative activities against three cancer cell lines in nanomolar concentrations. Interestingly, 7n' inhibited tubulin polymerization much more efficiently than CA-4. Cellular mechanism investigation elucidated 7n' disrupted the cellular microtubule structure, arrested cell cycle at G/M phase and induces apoptosis. Molecular modeling study revealed 1,2,5-oxadiazole-N-oxide ring could increase a hydrogen bond interaction with the binding site. These results provide impetus and further guidance for the development of new CA-4 analogues.
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hong2019designeuropean Use this key to autocite in the manuscript while using SciMatic Manuscript Manager or Thesis Manager
Authors Hong, Yilang;Zhao, Yinglin;Yang, Lei;Gao, Minghuan;Li, Long;Man, Shuai;Wang, Zhan;Guan, Qi;Bao, Kai;Zuo, Daiying;Wu, Yingliang;Zhang, Weige;
Journal European journal of medicinal chemistry
Year 2019
DOI
S0223-5234(19)30446-5
URL
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