Differential metabolism of 3FDT and docetaxel in RLMs, rats, and HLMs
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- 作者：Mei-Lin Tanga ; Lu Zhoub ; Jun Changa ; Zhuo-Han Huc ; Yan Qind ; qinyn11@126.com" class="auth_mail" title="E-mail the corresponding author ; Xun Suna ; e ; sunxunf@shmu.edu.cn" class="auth_mail" title="E-mail the corresponding author
- 关键词：3FDT ; Anticancer agents ; Cytochrome P450 ; Metabolites
- 刊名：European Journal of Medicinal Chemistry
- 出版年：2016
- 出版时间：4 May 2016
- 年：2016
- 卷：113
- 期：Complete
- 页码：81-91
- 全文大小：2326 K
文摘
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The C–F for C–H replacement at the C3′ group of docetaxel blocks its metabolism.
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The major metabolism site shifted from the C3′ group of docetaxel to the baccatin moiety of 3FDT.
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The main P450 switched from CYP3A for docetaxel to CYP3A and CYP2E1 for 3FDT.