2. Academic Validation
  3. Synthesis and anticancer activities of novel 1,2,4-triazolo[3,4-a]phthalazine derivatives

Synthesis and anticancer activities of novel 1,2,4-triazolo[3,4-a]phthalazine derivatives

  • Eur J Med Chem. 2014 Oct 6:85:235-44. doi: 10.1016/j.ejmech.2014.07.031.
Deng-Qi Xue 1,  Xu-Yao Zhang 1,  Chao-Jie Wang 1,  Li-Ying Ma 1,  Nan Zhu 1,  Peng He 1,  Kun-Peng Shao 1,  Peng-Ju Chen 1,  Yi-Fei Gu 1,  Xiao-Song Zhang 1,  Cai-Feng Wang 1,  Cong-Hui Ji 1,  Qiu-Rong Zhang 2,  Hong-Min Liu 3
Affiliations

Affiliations

  • 1 New Drug Research & Development Center, School of Pharmaceutical Sciences, Zhengzhou University, No. 100, KeXue DaDao, Zhengzhou 450001, China.
  • 2 New Drug Research & Development Center, School of Pharmaceutical Sciences, Zhengzhou University, No. 100, KeXue DaDao, Zhengzhou 450001, China. Electronic address: zqr406@sina.com.
  • 3 New Drug Research & Development Center, School of Pharmaceutical Sciences, Zhengzhou University, No. 100, KeXue DaDao, Zhengzhou 450001, China. Electronic address: liuhm@zzu.edu.cn.
PMID: 25086915 DOI: 10.1016/j.ejmech.2014.07.031
Abstract

Trying to develop potent and selective Anticancer agents, two series of novel 1,2,4-triazolo[3,4-a]phthalazine derivatives were designed and synthesized. Their antitumor activities were evaluated by MTT method against four selected human Cancer cell lines (MGC-803, EC-9706, HeLa and MCF-7). Our results showed that compound 11h exhibited good Anticancer activities compared to 5-fluorouracil against the four tested cell lines, with IC50 values ranging from 2.0 to 4.5 μM. Flow cytometry analysis indicated that compound 11h induced the cellular early Apoptosis and cell cycle arrest at G2/M phase in EC-9706.

Keywords

Anticancer; Apoptosis; Cell cycle arrest; Phthalazine; Triazole.

Figures