2. Academic Validation
  3. Synthesis and biological evaluation of N-substituted 3-oxo-1,2,3,4-tetrahydro-quinoxaline-6-carboxylic acid derivatives as tubulin polymerization inhibitors

Synthesis and biological evaluation of N-substituted 3-oxo-1,2,3,4-tetrahydro-quinoxaline-6-carboxylic acid derivatives as tubulin polymerization inhibitors

  • Eur J Med Chem. 2018 Jan 1:143:8-20. doi: 10.1016/j.ejmech.2017.08.018.
Jianguo Qi 1,  Haiyang Dong 1,  Jing Huang 1,  Shufeng Zhang 1,  Linqiang Niu 1,  Yahong Zhang 2,  Jianhong Wang 3
Affiliations

Affiliations

  • 1 Key Laboratory of Natural Medicine and Immuno-Engineering of Henan Province, Henan University Jinming Campus, Kaifeng, 475004, Henan, China.
  • 2 Key Laboratory of Natural Medicine and Immuno-Engineering of Henan Province, Henan University Jinming Campus, Kaifeng, 475004, Henan, China. Electronic address: zhangyahong_131@163.com.
  • 3 Key Laboratory of Natural Medicine and Immuno-Engineering of Henan Province, Henan University Jinming Campus, Kaifeng, 475004, Henan, China. Electronic address: jhworg@126.com.
PMID: 29172084 DOI: 10.1016/j.ejmech.2017.08.018
Abstract

A series of novel N-substituted 3-oxo-1,2,3,4-tetrahydro-quinoxaline-6-carboxy- lic acid derivatives were synthesized and evaluated for their biological activities. Among all synthesized target compounds, 13d exhibited the most potent antiproliferative activity against HeLa, SMMC-7721, K562 cell line (IC50 = 0.126 μM, 0.071 μM, 0.164 μM, respectively). Furthermore, compound 13d inhibited tubulin polymerization (IC50 = 3.97 μM), arrested cell cycle at the G2/M phase and induced Apoptosis. The binding mode at the colchicine binding site was also probed. These studies provided a new molecular scaffold for the further development of antitumor agents that target tubulin.

Keywords

3-Oxo-1,2,3,4-tetrahydro-quinoxaline-6-carboxylic acid derivatives; Antiproliferative; Cell apoptosis; Cell cycle analysis; Tubulin polymerization inhibitors.

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