Synthesis, biological evaluation, and molecular docking studies of 2-chloropyridine derivatives possessing 1,3,4-oxadiazole moiety as potential antitumor agents

  • Bioorg Med Chem. 2010 Nov 15;18(22):7836-41. doi: 10.1016/j.bmc.2010.09.051.
Qing-Zhong Zheng  1 ,  Xiao-Min Zhang ,  Ying Xu ,  Kui Cheng ,  Qing-Cai Jiao ,  Hai-Liang Zhu
Affiliations
  • 1. State Key Laboratory of Pharmaceutical Biotechnology, Nanjing University, Nanjing 210093, People's Republic of China.
PMID: 20947362 DOI: 10.1016/j.bmc.2010.09.051
Abstract

A series of new 2-chloropyridine derivatives possessing 1,3,4-oxadiazole moiety were synthesized. Antiproliferative assay results indicated that compounds 6o and 6u exhibited the most potent activity against gastric Cancer cell SGC-7901, which was more potent than the positive control. Especially, compound 6o exhibited significant Telomerase inhibitory activity (IC(50)=2.3±0.07μM), which was comparable to the positive control ethidium bromide. Docking simulation was performed to position compound 6o into the active site of Telomerase (3DU6) to determine the probable binding model.