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Paper | Regular issue | Vol 92, No. 11, 2016, pp.2018-2031
Published online, 27th September, 2016
DOI: 10.3987/COM-16-13548
Synthesis and Evaluation of the Antitumor Activities of Two Series of Jaspine B Analogues Bearing 2-Alkyloxymethyl Group

En Zhang,* Shang Wang, Jie Gao, Xiao-Jing Shi, Ming-Ming Wang, Shuai-Min Xu, and Hong-Min Liu*

*School of Pharmaceutical Sciences, Zhengzhou University, Ke xue DaDao 100, Zhengzhou 450001, China


Two series of jaspine B analogues bearing 2-alkyloxymethyl group have been synthesized and evaluated for their cytotoxicity against four cancer cell lines, including Eca-109, EC-9706, B16-F10 and MCF-7 cells. Most of the compounds exhibited potent cytotoxic activity against all four cell lines. The results also revealed that some of the analogues prepared in the current study exhibited comparable or better in vitro antitumor activity to jaspine B. Compound 9g, in particular, displayed the most potent antitumor activity of all of the compounds prepared in the current study with an IC50 value of 2.0 ± 0.4 μM towards B16-F10 cells, which was better than that of jaspine B (IC50 = 5.08 ± 0.6 μM). The results of a structure–activity relationship study showed that the oxygen atom and the length of the alkyl chain have an effect on the cytotoxic activity of these compounds.