2. Academic Validation
  3. Synthesis and antitumor activities of novel α-aminophosphonate derivatives containing an alizarin moiety

Synthesis and antitumor activities of novel α-aminophosphonate derivatives containing an alizarin moiety

  • Eur J Med Chem. 2014 Aug 18:83:116-28. doi: 10.1016/j.ejmech.2014.02.067.
Man-Yi Ye 1,  Gui-Yang Yao 2,  Ying-Ming Pan 1,  Zhi-Xin Liao 2,  Ye Zhang 3,  Heng-Shan Wang 4
Affiliations

Affiliations

  • 1 State Key Laboratory Cultivation Base for the Chemistry and Molecular Engineering of Medicinal Resources, School of Chemistry & Pharmaceutical Science of Guangxi Normal University, Yucai Road 15, Guilin 541004, Guangxi, PR China.
  • 2 Department of Pharmaceutical Engineering, School of Chemistry and Chemical Engineering, Southeast University, Nanjing 211189, PR China.
  • 3 State Key Laboratory Cultivation Base for the Chemistry and Molecular Engineering of Medicinal Resources, School of Chemistry & Pharmaceutical Science of Guangxi Normal University, Yucai Road 15, Guilin 541004, Guangxi, PR China; Department of Chemistry & Pharmaceutical Science, Guilin Normal College, Xinyi Road 15, Guangxi 541001, PR China. Electronic address: zhangye81@126.com.
  • 4 State Key Laboratory Cultivation Base for the Chemistry and Molecular Engineering of Medicinal Resources, School of Chemistry & Pharmaceutical Science of Guangxi Normal University, Yucai Road 15, Guilin 541004, Guangxi, PR China. Electronic address: whengshan@163.com.
PMID: 24953029 DOI: 10.1016/j.ejmech.2014.02.067
Abstract

A series of novel α-aminophosphonate derivatives containing an alizarin moiety (6-7) was designed and synthesized as antitumor agents. MTT (3-(4, 5-dimethylthiazol-2-yl)-2, 5-diphenyl tetrazolium bromide) assay results indicated that most compounds exhibited moderate to high inhibitory activity against KB, NCI-H460, HepG 2, A549, MGC-803, Hct-116, CNE and Hela tumor cell lines. The action mechanism of representative compounds 7h, 7j and 7n were investigated by fluorescence staining assays, flow cytometric analysis and real-time polymerase chain reaction (PCR) assays, which indicated that these compounds induced Apoptosis and involved G1 phase arrest by increasing the production of intracellular CA(2+) and Reactive Oxygen Species (ROS) and affecting associated Enzymes and genes. The results demonstrated that these compounds may induce Apoptosis through a mitochondrion-dependent pathway.

Keywords

Alizarin; Apoptosis; Cytotoxicity; Mitochondrial pathway; α-Aminophosphonate.

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