biostudies-literatureLi DDepartment of Natural Resources of Guangdong ProvinceNational Natural Science Foundation of China158https://www.ebi.ac.uk/biostudies/studies/S-EPMC8949366biostudies-literatureUnknown20(3)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.Marine drugsSynthesis of Marine Cyclopeptide Galaxamide Analogues as Potential Anticancer Agents.PMC8949366GDNRC [2020] 0372018YFC031090041876145, 81874292, 21672084GDNRC [2021] 482019YFD0901905202102010066, 201704030042Li DZhong SZhao BLiao XXu SfalseSynthesis of Marine Cyclopeptide Galaxamide Analogues as Potential Anticancer Agents.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.2022-01-01T00:00:00Z2022 Feb2025-04-04T14:49:53.815Z2025-04-04T14:49:53.815ZS-EPMC89493663532345710.3390/md20030158