Design, synthesis and biological evaluation of novel indole-based oxalamide and aminoacetamide derivatives as tubulin polymerization inhibitors.

Peng-Cheng Diao, Xie-Er Jian, Peng Chen, Chuan Huang, Jie Yin, Jie Chun Huang, Jun-Sheng Li, Pei-Liang Zhao

Bioorganic & medicinal chemistry letters 2020 Jan 15

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A series of novel indole-based oxalamide and aminoacetamide derivatives were designed, synthesized, and evaluated for antiproliferative activities. Preliminary results revealed that compound 8g exhibited significant antiproliferative effect against PC-3, HeLa and HCT-116 cell lines. Flow cytometric analysis of the cell cycle demonstrated the compound 8g induced the cell cycle arrest at G2/M phase in HeLa cell lines. Immunocytochemistry revealed loss of intact microtubule structure in cells treated with 8g andinhibition of tubulinpolymerization. Additionally, molecular docking analysis suggested that 8g formed stable interactions in the colchicine-binding site of tubulin. These preliminary results demonstrated that a new class of novel indole-based oxalamide and aminoacetamide derivatives described in the investigation could be developed as potential scaffolds to new anticancer agents. Copyright © 2019 Elsevier Ltd. All rights reserved.

Citation

Peng-Cheng Diao, Xie-Er Jian, Peng Chen, Chuan Huang, Jie Yin, Jie Chun Huang, Jun-Sheng Li, Pei-Liang Zhao. Design, synthesis and biological evaluation of novel indole-based oxalamide and aminoacetamide derivatives as tubulin polymerization inhibitors. Bioorganic & medicinal chemistry letters. 2020 Jan 15;30(2):126816