Anticancer Drugs (VI)——Synthesis and Activity of Spin Labeled Derivatives of 4-Amino-4-deoxy-4′-demethylepipodophyllotoxin

Chemical Research in Chinese Universities ›› 1996, Vol. 12 ›› Issue (3): 304-308.

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Anticancer Drugs (VI)——Synthesis and Activity of Spin Labeled Derivatives of 4-Amino-4-deoxy-4′-demethylepipodophyllotoxin

TIAN Xuan¹, YANG Ming-gui¹, JI Zhu-sheng and CHEN Yao-zu¹, HE Xiao-qing¹, LEI Xiao-hong², HAN Rui²

1. National Laboratory of Applied Organic Chemistry, Lanzhou Umversity, Lanzhou, 730000;
2. Institute of Materia Medica, Chinese Academy of Sciences, Beijing, 100050

Received:1995-12-12 Online:1996-07-15 Published:2011-11-18
Supported by:
Supported by Natural Science Foundation of Gansu Province

Abstract

Abstract: Some derivatives of podophyllotoxin(1), such as etoposide(12), possess antitumor activity and have been extensively used clinically^[1]. Because etoposide has a less solubility in water and higher toxicity, many chemists have an interest in further studies on the modification of the C-4 substituent of 1 for its better antitumor activity. Lee Kuo-hsing, Wang Zhe-qing et al. have synthesized a series of derivatives of CA (substituted anilino)-4-deoxypodophllotoxin. The pharmaceutical tests have shown that a number of 4β-(arylamino )-4'-demethylepi-podophyllotoxin are as potent as or more potent than etoposide(12) in inhibiting the human DNA topoisomerase Ⅱ.

Key words: 4-Amino-4-deoxy-4'-demethylepipodophyllotoxin, Nitroxyl radical, Anticancer activity

TIAN Xuan, YANG Ming-gui, JI Zhu-sheng and CHEN Yao-zu, HE Xiao-qing, LEI Xiao-hong, HAN Rui. Anticancer Drugs (VI)——Synthesis and Activity of Spin Labeled Derivatives of 4-Amino-4-deoxy-4′-demethylepipodophyllotoxin[J]. Chemical Research in Chinese Universities, 1996, 12(3): 304-308.

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Anticancer Drugs (VI)——Synthesis and Activity of Spin Labeled Derivatives of 4-Amino-4-deoxy-4′-demethylepipodophyllotoxin

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