Combating P-glycoprotein-mediated multidrug resistance with 10-O-phenyl dihydroartemisinin ethers in MCF-7 cells
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- 作者：Hang Zhonga ; Xuan Zhaob ; Zhizhong Zuoa ; Jingwei Suna ; Yao Yaoa ; Tao Wangb ; Dan Liua ; sammyld@163.com" class="auth_mail" title="E-mail the corresponding author ; Linxiang Zhaoa ; linxiang.zhao@vip.sina.com" class="auth_mail" title="E-mail the corresponding author
- 关键词：10-O-phenyl dihydroartemisinin ethers ; Multidrug-resistance ; MCF-7/Adr ; P-glycoprotein ; MDCK-MDR1 ; Antiproliferative effects ; Collateral sensitivity
- 刊名：European Journal of Medicinal Chemistry
- 出版年：2016
- 出版时间：27 January 2016
- 年：2016
- 卷：108
- 期：Complete
- 页码：720-729
- 全文大小：935 K
文摘
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A series of novel DHA derivatives characterized by 10-β-aryl substitution was synthesized.
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Novel compounds were more potent than positive control adriamycin against MDR cancer cells.
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P-gp-overexpressed MCF-7/Adr cells revealed collateral sensitivity towards novel compounds.
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MDCK-MDR1 assay indicated 3d and 5c could not be pumped by P-gp.
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Compound 5c aroused cell cycle arrest at G1 phase in MCF-7 and MCF-7/Adr cells.