Synthesis and anticancer activity evaluation of a series of [1,2,4]triazolo[1,5-a]pyridinylpyridines in vitro and in vivo

  • Eur J Med Chem. 2013 Sep:67:243-51. doi: 10.1016/j.ejmech.2013.06.052.
Xiao-Meng Wang  1 ,  Jing Xu ,  Yi-Ping Li ,  Huan Li ,  Cong-Shan Jiang ,  Guang-De Yang ,  She-Min Lu ,  San-Qi Zhang
Affiliations
  • 1. Department of Medicinal Chemistry, School of Pharmacy, Health Science Center, Xi'an Jiaotong University, Xi'an 710061, PR China.
PMID: 23871904 DOI: 10.1016/j.ejmech.2013.06.052
Abstract

A series of [1,2,4]triazolo[1,5-a]pyridinylpyridines were synthesized and characterized. Their antiproliferative activities in vitro were evaluated by MTT against three human Cancer cell lines including HCT-116, U-87 MG and MCF-7 cell lines. The SAR of target compounds was preliminarily discussed. The compounds 1c and 2d with potent antiproliferative activities were tested for their effects on the Akt and p-AKT(473). The Anticancer effect of 1c was evaluated in mice bearing sarcoma S-180 model. The results suggest that the title compounds are potent Anticancer agents.

Keywords
Anticancer effect; Antiproliferative activities; Synthesis; [1,2,4]Triazolo[1,5-a]pyridine.