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

Index: Bioorg. Med. Chem. 18 , 7836-41, (2010)

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Abstract

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.