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Antitumor agents. 78. Inhibition of human DNA topoisomerase II by podophyllotoxin and alpha-peltatin analogues.

作者信息

Thurston L S, Irie H, Tani S, Han F S, Liu Z C, Cheng Y C, Lee K H

出版信息

J Med Chem. 1986 Aug;29(8):1547-50. doi: 10.1021/jm00158a042.

DOI:10.1021/jm00158a042
PMID:3016271
Abstract

It has been reported that the action of etoposide (VP-16) (14) as an antitumor agent is mediated through its interaction with DNA topoisomerase II which results in DNA breakage inside the cell. In order to understand the mechanism of action as well as structure-activity relationships of 14, several novel, synthetic and some naturally occurring analogues related to podophyllotoxin were examined for inhibition of the DNA topoisomerase II activity. Compound 2 exhibited enhanced activity and compound 5 slightly diminished activity relative to 14. A 4 beta-substituted ether at the C ring and O-demethylation at the E ring appear to enhance activity.

摘要

相似文献

1
Antitumor agents. 78. Inhibition of human DNA topoisomerase II by podophyllotoxin and alpha-peltatin analogues.
J Med Chem. 1986 Aug;29(8):1547-50. doi: 10.1021/jm00158a042.
2
Antitumor agents. 100. Inhibition of human DNA topoisomerase II by cytotoxic ether and ester derivatives of podophyllotoxin and alpha-peltatin.抗肿瘤剂。100. 鬼臼毒素和α-盾叶鬼臼素的细胞毒性醚类和酯类衍生物对人DNA拓扑异构酶II的抑制作用
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Antitumor agents, 99. Synthetic ring C aromatized podophyllotoxin analogues as potential inhibitors of human DNA topoisomerase II.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
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A rational design strategy of the novel topoisomerase II inhibitors for the synthesis of the 4-O-(2-pyrazinecarboxylic)-4'-demethylepipodophyllotoxin with antitumor activity by diminishing the relaxation reaction of topoisomerase II-DNA decatenation.一种新型拓扑异构酶II抑制剂的合理设计策略，用于合成具有抗肿瘤活性的4-O-(2-吡嗪羧酸)-4'-去甲基表鬼臼毒素，通过减少拓扑异构酶II-DNA解连环的松弛反应来实现。
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Antitumor agents. I. DNA topoisomerase II inhibitory activity and the structural relationship of podophyllotoxin derivatives as antitumor agents.抗肿瘤剂。I. 作为抗肿瘤剂的鬼臼毒素衍生物的DNA拓扑异构酶II抑制活性及其结构关系。
Chem Pharm Bull (Tokyo). 1992 Oct;40(10):2720-7. doi: 10.1248/cpb.40.2720.
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Antitumor agents. 125. New 4 beta-benzoylamino derivatives of 4'-O-demethyl-4-desoxypodophyllotoxin and 4 beta-benzoyl derivatives of 4'-O-demethylpodophyllotoxin as potent inhibitors of human DNA topoisomerase II.抗肿瘤剂。125. 4'-O-去甲基-4-脱氧鬼臼毒素的新型4β-苯甲酰氨基衍生物和4'-O-去甲基鬼臼毒素的4β-苯甲酰衍生物作为人DNA拓扑异构酶II的有效抑制剂
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Antitumor agents. 126. Novel 4 beta-substituted anilino derivatives of 3',4'-O,O-didemethylpodophyllotoxin as potent inhibitors of human DNA topoisomerase II.抗肿瘤剂。126. 新型3'，4'-O，O-二去甲基鬼臼毒素的4β-取代苯胺衍生物作为人DNA拓扑异构酶II的有效抑制剂
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