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Synthesis and biological evaluation of berberine derivatives bearing 4-aryl-1-piperazine moieties

机译:带有4-芳基-1-哌嗪部分的小ber碱衍生物的合成及生物学评价

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摘要

Piperazine moieties with disubstituted N-aryl groups are linked to the isoquinoline alkaloid, berberine, through a pentyloxy side chain, replacing its 9-methoxyl group. The nine synthesised compounds are screened for antioxidant potency, in vitro anticancer activities against Hela and Caski cervical cancer cell lines and for cytotoxicity towards Malin Darby canine kidney cell lines. Several compounds demonstrate significant antioxidant potency and most of the compounds exhibit equipotent, or better, anticancer activity when compared to berberine.
机译:具有二取代的N-芳基的哌嗪部分通过戊氧基侧链连接到异喹啉生物碱小ber碱,取代了其9-甲氧基。筛选了九种合成的化合物的抗氧化剂效能,针对Hela和Caski宫颈癌细胞系的体外抗癌活性以及针对Malin Darby犬肾细胞系的细胞毒性。与小ber碱相比,几种化合物显示出显着的抗氧化剂功效,并且大多数化合物具有同等或更佳的抗癌活性。

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