Bioorganic & Medicinal Chemistry 2010-01-01

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

Qing-Zhong Zheng, Xiao-Min Zhang, Ying Xu, Kui Cheng, Qing-Cai Jiao, Hai-Liang Zhu, Qing-Zhong Zheng, Xiao-Min Zhang, Ying Xu, Kui Cheng, Qing-Cai Jiao, Hai-Liang Zhu

文献索引：Bioorg. Med. Chem. 18 , 7836-41, (2010)

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摘要

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 ± 0.07 μM), 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.

相关化合物

  • 溴化乙啶
  • 5-氟尿嘧啶
  • 2-氯吡啶

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