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二茂铁基鬼臼毒素缀合物的合成与生物性质评价。

Synthesis and evaluation of biological properties of ferrocenyl-podophyllotoxin conjugates.

机构信息

Department of Organic Chemistry, Faculty of Chemistry, University of Łódź, Tamka 12, 91-403 Łódź, Poland.

出版信息

Dalton Trans. 2017 Aug 22;46(33):10847-10858. doi: 10.1039/c7dt02107k.

Abstract

Three types, esters, amides and 1,2,3-triazoles, of ferrocenyl-podophyllotoxin conjugates were synthesised, and their anticancer activity was evaluated. We observed that the most potent ferrocenyl derivatives were esters. Esters 15, 16 and 17 acted in a similar way to podophyllotoxin, i.e. reduced the number of G1 phase cells and induced G2/M blockage, while esters 14 and 18 and amide 19 blocked cells in S phase in a similar manner to etoposide.

摘要

合成了三种类型的二茂铁基鬼臼毒素缀合物,酯、酰胺和 1,2,3-三唑,并评估了它们的抗癌活性。我们观察到最有效的二茂铁衍生物是酯。酯 15、16 和 17 的作用方式与鬼臼毒素相似,即减少 G1 期细胞数量并诱导 G2/M 阻滞,而酯 14 和 18 以及酰胺 19 则以类似于依托泊苷的方式将细胞阻滞在 S 期。

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