2. Academic Validation
  3. Design, synthesis and pharmacological evaluation of new 2-oxo-quinoline derivatives containing α-aminophosphonates as potential antitumor agents

Design, synthesis and pharmacological evaluation of new 2-oxo-quinoline derivatives containing α-aminophosphonates as potential antitumor agents

  • Medchemcomm. 2017 Mar 31;8(6):1158-1172. doi: 10.1039/c7md00098g.
Yan-Cheng Yu 1 2,  Wen-Bin Kuang 2,  Ri-Zhen Huang 2,  Yi-Lin Fang 2,  Ye Zhang 1 2 3,  Zhen-Feng Chen 2,  Xian-Li Ma 1
Affiliations

Affiliations

  • 1 College of Pharmacy , Guilin Medical University , Guilin 541004 , PR China . Email: zhangye81@126.com ; Email: mxl78@glmc.edu.cn ; ; Tel: +86 773 5895132.
  • 2 State Key Laboratory for the Chemistry and Molecular Engineering of Medicinal Resources (Ministry of Education of China) , School of Chemistry and Pharmaceutical Sciences of Guangxi Normal University , Guilin 541004 , PR China . Email: chenzf@gxnu.edu.cn.
  • 3 Department of Chemistry & Pharmaceutical Science , Guilin Normal College , Guilin 541001 , PR China.
PMID: 30108826 DOI: 10.1039/c7md00098g
Abstract

A series of novel 2-oxo-quinoline derivatives containing α-aminophosphonates were designed and synthesized as antitumor agents. MTT (3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide) assay results demonstrated that some compounds exhibited moderate to high inhibitory activity against HepG2, SK-OV-3 and NCI-H460 tumor cell lines, and most compounds showed much lower cytotoxicity against HL-7702 normal cells than 5-FU and cisplatin. The action mechanism of representative compound 5b was investigated by fluorescence staining assay, flow cytometric analysis and western blot (WB) assay, which indicated that this compound induced Apoptosis and G2/M phase arrest accompanied by an increase in the production of intracellular CA2+ and Reactive Oxygen Species (ROS) and affecting associated Enzymes and genes.

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