Synthesis of Marine Cyclopeptide Galaxamide Analogues as Potential Anticancer Agents
Daichun Li; Xiaojian Liao; Shenghui Zhong; Bingxin Zhao; Shihai Xu
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) &mu:g/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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