Yu Peng-Fei, Chen Hong, Wang Jing, He Chun-Xian, Cao Bo, Li Min, Yang Na, Lei Zhi-Yong, Cheng Mao-Sheng
Key Lab of New Drugs Design and Discovery of Liaoning Province, School of Pharmaceutical Engineering, Shenyang Pharmaceutical University, Shenyang, China.
Chem Pharm Bull (Tokyo). 2008 Jun;56(6):831-4. doi: 10.1248/cpb.56.831.
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.
采用联合策略设计了一系列新型鬼臼毒素衍生物，并通过将鬼臼毒素（1）或4β-氨基鬼臼毒素（3）与取代的吲哚-3-基-氯乙醛偶联来合成这些衍生物。利用光谱技术确定了它们的结构。与母体化合物1、3和indibulin（2）相比，对这些新型衍生物进行了体外对四种人类癌细胞系的细胞毒性评估。一些化合物（7a、7c）显示出与鬼臼毒素相当的细胞毒性。
