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Bioorg Med Chem Lett. 2015 Mar 1;25(5):1067-71. doi: 10.1016/j.bmcl.2015.01.011. Epub 2015 Jan 13.

Discovery of phenylpiperazine derivatives as IGF-1R inhibitor with potent antiproliferative properties in vitro.

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School of Life Sciences, Shandong University of Technology, Zibo 255049, Shandong Province, PR China.


A series of phenylpiperazine derivatives (3a-3q) were designed and synthesized. In vitro assays indicated that several phenylpiperazine derivatives had excellent antiproliferative properties against four cancer cell lines including multidrug-resistant cancer cell lines, with IC50 values in the low micromolar range. The average IC50 of the most active compound 3b is 0.024μM to the MCF-7 cell line. In addition, the mechanism of action of these new analogues was investigated by molecular docking studies, insulin-like growth factor 1-receptor (IGF-1R) kinase assay and apoptosis induced assay. These studies confirmed that these new phenylpiperazine derivatives maintain their mechanisms of action by disrupting IGF-1R kinase.


Apoptosis; Computer simulation; IGF-1R inhibitors; Phenylpiperazine

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