4-aza-2,3-dehydro-4-deoxypodophyllotoxins: Simple aza-podophyllotoxin analogues possessing potent cytotoxicity

被引：77

作者：

Hitotsuyanagi, Y ^{[1
]}

Fukuyo, M ^{[1
]}

Tsuda, K ^{[1
]}

Kobayashi, M ^{[1
]}

Ozeki, A ^{[1
]}

Itokawa, H ^{[1
]}

Takeya, K ^{[1
]}

机构：

[1] Tokyo Univ Pharm & Life Sci, Hachioji, Tokyo 1920392, Japan

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2000年 / 10卷 / 04期

关键词：

D O I：

10.1016/S0960-894X(99)00693-9

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

4-Aza-2,3-dehydro-4-deoxypodophyllotoxin analogues 3a-n were synthesized through quinolines 2a-n. Comparison of their cytotoxicity against P-388 leukemia cells revealed that the steric effects of the ring B substituents on the activity are greater than the electronic effects, while the presence of a methoxy group on the ring E is not essential to exhibit potent cytotoxicity. Analogues 3a and 3b proved to be more than twice as cytotoxic as natural podophyllotoxin (1). (C) 2000 Elsevier Science Ltd. All rights reserved.

引用

页码：315 / 317

页数：3

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