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高等学校化学研究 ›› 1993, Vol. 9 ›› Issue (2): 116-120.

• Articles • 上一篇    下一篇

Anticancer Drugs (Ⅳ)——New Derivatives of Podophyllotoxin

TIAN Xuan1, LI Jin-xin1, ZHANG Ya-li1, CHEN Yao-zu1, LI Wen-guang2   

  1. 1. National Laboratory of Applied Organic Chemistry, Lanzhou University, Lanzhou, 730000;
    2. Department of Pharmacology, Lanzhou Medicine College, Lanzhou, 730000
  • 收稿日期:1992-03-03 出版日期:1993-04-24 发布日期:2011-08-17

Anticancer Drugs (Ⅳ)——New Derivatives of Podophyllotoxin

TIAN Xuan1, LI Jin-xin1, ZHANG Ya-li1, CHEN Yao-zu1, LI Wen-guang2   

  1. 1. National Laboratory of Applied Organic Chemistry, Lanzhou University, Lanzhou, 730000;
    2. Department of Pharmacology, Lanzhou Medicine College, Lanzhou, 730000
  • Received:1992-03-03 Online:1993-04-24 Published:2011-08-17

摘要: Four new derivatives of podophyllotoxin, N’-podophyllic acid-N-[3-(2, 2, 5, 5-te-tramethyl-pyrrolinenyloxy)] semicarbazide(GP-11, 6), podophyllic acid [3-(2,2,5,5-te-tramethyl-pyrrolinenyloxy)]hydrazone (GP-12, 7), podophyllic acid-[4-(2, 2, 6, 6-tetramethyl-1-hydroxy piperidine)]hydrazone(GP-1-OH, 8) and podophyllic acid[4-(2,2, 6, 6-tetramethyl piperidine)]hydrazone(GP-1-H, 9) were synthesized. The inhibition effect of the four new compounds on L-1210 cells were determined. The antitumor activity and toxicity of GP-1(2), GP-1-OH(8), GP-1-H(9) and VP-16-213(1) were discussed.

关键词: Podophyllotoxin, Anticancer drugs, Nitroxyl radical

Abstract: Four new derivatives of podophyllotoxin, N’-podophyllic acid-N-[3-(2, 2, 5, 5-te-tramethyl-pyrrolinenyloxy)] semicarbazide(GP-11, 6), podophyllic acid [3-(2,2,5,5-te-tramethyl-pyrrolinenyloxy)]hydrazone (GP-12, 7), podophyllic acid-[4-(2, 2, 6, 6-tetramethyl-1-hydroxy piperidine)]hydrazone(GP-1-OH, 8) and podophyllic acid[4-(2,2, 6, 6-tetramethyl piperidine)]hydrazone(GP-1-H, 9) were synthesized. The inhibition effect of the four new compounds on L-1210 cells were determined. The antitumor activity and toxicity of GP-1(2), GP-1-OH(8), GP-1-H(9) and VP-16-213(1) were discussed.

Key words: Podophyllotoxin, Anticancer drugs, Nitroxyl radical