Synthesis of Marine Cyclopeptide Galaxamide Analogues as Potential Anticancer Agents |
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| Authors: | Daichun Li Xiaojian Liao Shenghui Zhong Bingxin Zhao Shihai Xu |
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| Institution: | Department of Chemistry, College of Chemistry and Materials Science, Jinan University, Guangzhou 510632, China; (D.L.); (X.L.); (S.Z.) |
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| Abstract: | In this paper, eight new galaxamide analogues (Z-1~Z-8) were synthesized and evaluated for their cytotoxic activities against five cancer cell lines, MCF-7, MD-MBA-231, HepG2, Hela, and A549, using MTT assays. The modified analogue Z-6 displayed broad spectrum cytotoxic activity toward each tested cell line with IC50 values of 1.65 ± 0.30 (MCF-7), 2.91 ± 0.17 (HepG2), 4.59 ± 0.27 (MD-MBA-231), 5.69 ± 0.37 (Hela), and 5.96 ± 0.41 (A549) μg/mL, respectively. The galaxamides Z-3 and Z-6 induced concentration-dependent apoptosis of the MCF-7 cells after 72 h as evaluated by the flow cytometry experiment. The results showed that these compounds could induce MCF-7 cell apoptosis by arresting the G0/G1 phase of the cell cycle and finally achieving the effect of inhibiting the proliferation of MCF-7 cells. |
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| Keywords: | drug design anticancer apoptosis cyclic pentapeptide galaxamide analogues |
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