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• W4309264787 abstract "Abstract The mitochondria are the energy and biosynthesis factory and the majority source of reactive oxygen species (ROS). The mitochondria play a vital role in carcinogenesis, so the mitochondria targeting drugs have been the focus of new drug discovery in cancer therapy. In this study, target mitochondrial stilbene compounds A1-A6 are synthesized by introducing lipophilic cationic triphenylphosphonium into the pharmacophore. Intriguingly, the strategy significantly improved the anticancer potential of parent resveratrol. Especially A4 (( E )-Triphenyl(4-(4-(3,4 dimethylstyryl)phenoxy)butyl)phosphoniumiodide) exerted the excellent anticancer activity in HeLa cells. The mechanism study showed that A4 could effectively decrease cyclin D1/cyclin E1 level to arrest the cell cycle in G0/G1, and target the mitochondria to induce apoptosis referring the cross-talk of the decreased ATPase activity, elevated ROS and increased cytosolic Ca 2+ to inhibit tumor cell proliferation. Overall, this study is evidence that the target mitochondria drug discovery is an excellent strategy for exploiting the drug potential in cancer therapy." @default.
• W4309264787 created "2022-11-25" @default.
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• W4309264787 date "2022-11-17" @default.
• W4309264787 modified "2023-09-24" @default.
• W4309264787 title "Methylated and mitochondria-targeted analogue of resveratrol with inhibition of tumor cell growth" @default.
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• W4309264787 doi "https://doi.org/10.21203/rs.3.rs-2274451/v1" @default.
• W4309264787 hasPublicationYear "2022" @default.
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