1. Synthesis and anticancer activity evaluation of a series of [1,2,4]triazolo[1,5-a]pyridinylpyridines in vitro and in vivo
- Author
-
Xiao-Meng Wang, Congshan Jiang, San-Qi Zhang, Jing Xu, Shemin Lu, Guang-De Yang, Huan Li, and Yi-Ping Li
- Subjects
Models, Molecular ,Pyridines ,Antineoplastic Agents ,Pharmacology ,Mice ,Structure-Activity Relationship ,In vivo ,Drug Discovery ,Tumor Cells, Cultured ,medicine ,Animals ,Humans ,Protein kinase B ,Cell Proliferation ,Dose-Response Relationship, Drug ,Molecular Structure ,Chemistry ,Organic Chemistry ,Neoplasms, Experimental ,General Medicine ,Triazoles ,HCT116 Cells ,medicine.disease ,In vitro ,Disease Models, Animal ,Cell culture ,MCF-7 Cells ,Cancer research ,Sarcoma ,Drug Screening Assays, Antitumor ,Human cancer - 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.
- Published
- 2013