抗肿瘤剂，99. 合成的C环芳构化鬼臼毒素类似物作为人类DNA拓扑异构酶II的潜在抑制剂
Antitumor agents, 99. Synthetic ring C aromatized podophyllotoxin analogues as potential inhibitors of human DNA topoisomerase II.
作者信息
Beers S A, Imakura Y, Dai H J, Li D H, Cheng Y C, Lee K H
机构信息
Division of Medicinal Chemistry and Natural Products, School of Pharmacy, University of North Carolina, Chapel Hill 27599.
出版信息
J Nat Prod. 1988 Sep-Oct;51(5):901-5. doi: 10.1021/np50059a014.
PMID:2849640
Abstract
Several ring C aromatized analogues of podophyllotoxin were synthesized for testing against human DNA topoisomerase II. The results indicate that aromatization of ring C gave rise to no inhibition of this enzyme at 200 microM. A comparison of the cytotoxicity among these compounds also demonstrates that a free hydroxyl group at C-4 contributes to significant cytotoxicity.
摘要
合成了几种鬼臼毒素的C环芳构化类似物，用于测试其对人DNA拓扑异构酶II的作用。结果表明，在200微摩尔浓度下，C环芳构化对该酶没有抑制作用。这些化合物细胞毒性的比较也表明，C-4位的游离羟基对显著的细胞毒性有作用。
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