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Synthesis and biological activity of C-7, C-9 and C-10 modified taxane analogues from 1-deoxybaccatin VI

Chenghu Xie, Yongmei Cui, Lanlan Li, Minmin Zhang, Hongchun Liu, Haixia Lin

BIOORGANIC & MEDICINAL CHEMISTRY(2020)

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摘要
A series of C-7, C-9 and C-10 modified taxane analogues were synthesized and their in vitro anticancer activities against three human cancer cell lines: A-549 (human lung cancer cell line), MDA-MB-231 (human breast cancer cell line), A-549/T (human lung cancer resistant cell line) were studied. The novel 1-deoxybaccatin VI derivatives modified with carbonate group at C-9 and C-10 positions enable the behavior of these compounds to be evidently distinct from other similar compounds. The strong cytotoxicity in the three cell lines, especially in drug-resistant cell line, showed by the newly synthesized taxane analogues indicated them as potential lead compounds for anticancer drug design.
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关键词
Paclitaxel,Taxane analogues,1-Deoxybaccatin VI,Synthesis,In vitro anticancer activity
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