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Original Vinca Derivatives: From P‑Glycoprotein Substrates to P‑Glycoprotein Inhibitors

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Figshare2016-11-23 更新2026-04-29 收录
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https://figshare.com/articles/dataset/Original_Vinca_Derivatives_From_P_Glycoprotein_Substrates_to_P_Glycoprotein_Inhibitors/4249640
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The first example of vinca derivatives 16–18 able to modulate P-glycoprotein (Pgp) efflux activity is reported. They were elaborated in two steps from vinorelbine 3 (VLN) by a modification of the velbenamine moiety. These compounds were able to decrease efficiently Pgp mediated influx and efflux of rhodamine-123 (Rho) and to restore the cytotoxicity of vinorelbine 3 (VLN) and doxorubicin (Dox) on K562R (dox-resistant) cell lines.
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2016-11-23
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