2. Academic Validation
  3. Design, synthesis and in vitro biological evaluation of novel [1,2,3]triazolo[4,5-d]pyrimidine derivatives containing a thiosemicarbazide moiety

Design, synthesis and in vitro biological evaluation of novel [1,2,3]triazolo[4,5-d]pyrimidine derivatives containing a thiosemicarbazide moiety

  • Eur J Med Chem. 2018 Feb 25:146:147-156. doi: 10.1016/j.ejmech.2018.01.031.
Peng-Fei Geng 1,  Xue-Qi Liu 1,  Tao-Qian Zhao 1,  Cong-Cong Wang 1,  Zhong-Hua Li 1,  Ji Zhang 1,  Hao-Ming Wei 1,  Biao Hu 1,  Li-Ying Ma 2,  Hong-Min Liu 3
Affiliations

Affiliations

  • 1 Collaborative Innovation Center of New Drug Research and Safety Evaluation, Henan Province, Key Laboratory of Technology of Drug Preparation (Zhengzhou University), Ministry of Education of China, Key Laboratory of Henan Province for Drug Quality and Evaluation, School of Pharmaceutical Sciences, Zhengzhou University, Zhengzhou, 450001, PR China.
  • 2 Collaborative Innovation Center of New Drug Research and Safety Evaluation, Henan Province, Key Laboratory of Technology of Drug Preparation (Zhengzhou University), Ministry of Education of China, Key Laboratory of Henan Province for Drug Quality and Evaluation, School of Pharmaceutical Sciences, Zhengzhou University, Zhengzhou, 450001, PR China. Electronic address: maliying@zzu.edu.cn.
  • 3 Collaborative Innovation Center of New Drug Research and Safety Evaluation, Henan Province, Key Laboratory of Technology of Drug Preparation (Zhengzhou University), Ministry of Education of China, Key Laboratory of Henan Province for Drug Quality and Evaluation, School of Pharmaceutical Sciences, Zhengzhou University, Zhengzhou, 450001, PR China. Electronic address: liuhm@zzu.edu.cn.
PMID: 29407946 DOI: 10.1016/j.ejmech.2018.01.031
Abstract

A series of hybrid molecules containing [1,2,3]triazolo[4,5-d]pyrimidine and thiosemicarbazide moieties were designed, synthesized and evaluated for their antiproliferative activities against MGC-803, NCI-H1650 and PC-3 human Cancer cells. Some of the synthesized compounds showed moderate to good activity against three selected Cancer cell lines. Among these compounds, compound 29 displayed the most potent antiproliferative activity as well as good selectivity between Cancer cells and normal cells. Further mechanism studies revealed that compound 29 could obviously inhibit the colony formation and migration of MGC-803 as well as induced Apoptosis.

Keywords

Antiproliferative activity; Pyrimidine; Thiosemicarbazide; Triazole.

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