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Eur J Med Chem. 2013 Sep;67:243-51. doi: 10.1016/j.ejmech.2013.06.052. Epub 2013 Jul 4.

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

Author information

1
Department of Medicinal Chemistry, School of Pharmacy, Health Science Center, Xi'an Jiaotong University, Xi'an 710061, PR China.

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

PMID:
23871904
DOI:
10.1016/j.ejmech.2013.06.052
[Indexed for MEDLINE]

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