Synthesis, biological evaluation, and molecular docking studies of 1,3,4-oxadiazole derivatives possessing 1,4-benzodioxan moiety as potential anticancer agents
2011
Zhang, Xiao-Min | Qiu, Min | Sun, Juan | Zhang, Yan-Bin | Yang, Yu-Shun | Wang, Xiao-Liang | Tang, Jian-Feng | Zhu, Hai-Liang
In present study, a series of new 1,3,4-oxadiazole derivatives containing 1,4-benzodioxan moiety (6a–6s) as potential telomerase inhibitors were synthesized. The bioassay tests demonstrated that compounds 6k, 6l, 6m, 6n and 6s exhibited broad-spectrum antitumor activity with IC₅₀ concentration range from 7.21μM to 25.87μM against the four cancer cell lines, HEPG2, HELA, SW1116 and BGC823. Moreover, all the title compounds were assayed for telomerase inhibition using the TRAP-PCR-ELISA assay. The results showed compound 6k possessed the most potent telomerase activity (IC₅₀=1.27±0.05μM). Docking simulation was performed to position compound 6k into the active site of telomerase (3DU6) to determine the probable binding model.
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