Synthesis and Anticancer Activity of Podophyllotoxin Derivatives

被引:2
作者
Lin, K. [1 ,2 ]
Zhang, X. [3 ]
Dai, X. [3 ]
Ma, L. [4 ]
Bozorov, K. [1 ,5 ]
Guo, H. [1 ,2 ]
Huang, G. [1 ,4 ]
Cao, J. [3 ]
机构
[1] Chinese Acad Sci, Xinjiang Tech Inst Phys & Chem, Key Lab Plant Resources & Chem Arid Zone, Urumqi 830011, Peoples R China
[2] Univ Chinese Acad Sci, Beijing 100049, Peoples R China
[3] Shanghai Normal Univ, Coll Life Sci, Shanghai 201418, Peoples R China
[4] Anhui Univ Technol, Coll Chem & Chem Engn, Maanshan 243002, Peoples R China
[5] Acad Sci Uzbek, Inst Chem Plant Subst, 77 Mirzo Ulugbek St, Tashkent 100170, Uzbekistan
关键词
lignan; podophyllotoxin; structural modification; anticancer activity; MCF-7; AGENTS;
D O I
10.1007/s10600-021-03539-z
中图分类号
R914 [药物化学];
学科分类号
100701 ;
摘要
Two series of podophyllotoxin derivatives were synthesized by addition of a 4 beta-sulfanilamide to or substitution of a 4 beta-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 mu M. A change in the morphology of MCF-7 cells treated with 9f also confirmed its activity as a cytotoxic derivative against cancer cells.
引用
收藏
页码:1010 / 1018
页数:9
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