2. Academic Validation
  3. Synthesis and biological evaluation of 4-(1,2,3-triazol-1-yl)coumarin derivatives as potential antitumor agents

Synthesis and biological evaluation of 4-(1,2,3-triazol-1-yl)coumarin derivatives as potential antitumor agents

  • Bioorg Med Chem Lett. 2014 Feb 1;24(3):799-807. doi: 10.1016/j.bmcl.2013.12.095.
Wenjuan Zhang 1,  Zhi Li 1,  Meng Zhou 1,  Feng Wu 1,  Xueyan Hou 1,  Hao Luo 1,  Hao Liu 1,  Xuan Han 1,  Guoyi Yan 1,  Zhenyu Ding 1,  Rui Li 2
Affiliations

Affiliations

  • 1 State Key Laboratory of Biotherapy and Cancer Center, West China Hospital, Sichuan University, Chengdu, 610041 Sichuan, PR China.
  • 2 State Key Laboratory of Biotherapy and Cancer Center, West China Hospital, Sichuan University, Chengdu, 610041 Sichuan, PR China. Electronic address: lirui@scu.edu.cn.
PMID: 24418772 DOI: 10.1016/j.bmcl.2013.12.095
Abstract

In this research, a series of 4-(1,2,3-triazol-1-yl)coumarin conjugates were synthesized and their Anticancer activities were evaluated in vitro against three human Cancer cell lines, including human breast carcinoma MCF-7 cell, colon carcinoma SW480 cell and lung carcinoma A549 cell. To increase the biological potency, structural optimization campaign was conducted focusing on the C-4 position of 1,2,3-triazole and the C-6, C-7 positions of coumarin. In addition, to further evaluate the role of 1,2,3-triazole and coumarin for antiproliferative activity, 9 compounds possessing 4-(piperazin-1-yl)coumarin framework and 3 derivatives baring quinoline core were also synthesized. By MTT assay in vitro, most of the compounds display attractive antitumor activities, especially 23. Further flow cytometry assays demonstrate that compound 23 exerts the antiproliferative role through arresting G2/M cell-cycle and inducing Apoptosis.

Keywords

1,2,3-Triazole; Antiproliferative activity; Apoptosis; Coumarin; G(2)/M cell-cycle arrest.

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