Synthesis and Anticancer Activity of Podophyllotoxin Derivatives

被引:0
作者
K. Lin
X. Zhang
X. Dai
L. Ma
K. Bozorov
H. Guo
G. Huang
J. Cao
机构
[1] Chinese Academy of Sciences,Key Laboratory of Plant Resources and Chemistry of Arid Zone, Xinjiang Technical Institute of Physics and Chemistry
[2] University of Chinese Academy of Sciences,College of Life Sciences
[3] Shanghai Normal University,College of Chemistry and Chemical Engineering
[4] Anhui University of Technology,Institute of Chemistry of Plant Substances
[5] Academy of Sciences of Uzbekistan,undefined
来源
Chemistry of Natural Compounds | 2021年 / 57卷
关键词
lignan; podophyllotoxin; structural modification; anticancer activity; MCF-7;
D O I
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中图分类号
学科分类号
摘要
Two series of podophyllotoxin derivatives were synthesized by addition of a 4β-sulfanilamide to or substitution of a 4β-amide into podophyllotoxin. Their cytotoxicities were evaluated against four human cancer cell lines (A549, HeLa, MCF-7, and PC-3). Investigations of the structure–activity relationship were generalized. Derivative 9f (2-thienoylaminoepipodophyllotoxin) exhibited the highest activity against the cancer cells, inhibiting growth of MCF-7 cells with IC50 0.67 ± 0.37 μM. A change in the morphology of MCF-7 cells treated with 9f also confirmed its activity as a cytotoxic derivative against cancer cells.
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页码:1010 / 1018
页数:8
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