Original Vinca Derivatives: From P-Glycoprotein Substrates to P-Glycoprotein Inhibitors
详细信息 查看全文
- 作者：Olga Gherbovet ; María Concepción García Alvarez ; Jérôme Bignon ; Fanny Roussi
- 刊名：Journal of Medicinal Chemistry
- 出版年：2016
- 出版时间：December 8, 2016
- 年：2016
- 卷：59
- 期：23
- 页码：10774-10780
- 全文大小：408K
- ISSN：1520-4804
文摘
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.