Design, Synthesis and Cytotoxicity of Novel Podophyllotoxin Derivatives

作者：Pengfei Yu, Hong Chen, Jing Wang, Chun‐Xian He, Bo Cao, Min Li, Na Yang, Zhiyong Lei, Maosheng Cheng · 发表于：Chemical and Pharmaceutical Bulletin · 年份：2008 · DOI：10.1248/cpb.56.831 · 被引用次数：34 · 研究领域：Plant-derived Lignans Synthesis and Bioactivity、Cancer Treatment and Pharmacology、Biological Activity of Diterpenoids and Biflavonoids

A series of novel podophyllotoxin derivatives were designed using association strategy and synthesized by coupling either podophyllotoxin (1) or 4beta-amino podophyllotoxin (3) with substituted indol-3-yl-glyoxyl chlorides. Their structures were identified using spectroscopic techniques. These novel derivatives have been evaluated for cytotoxicity in vitro against four human cancer cell lines with comparison to the parent compounds 1, 3 and indibulin (2). Some of the compounds (7a, 7c) showed comparable cytotoxicity to that of podophyllotoxin.