Synthesis and biological activities of topoisomerase I inhibitors, 6-N-amino analogues of NB-506

被引：20

作者：

Ohkubo, M ^{[1
]}

Kojiri, K ^{[1
]}

Kondo, H ^{[1
]}

Tanaka, S ^{[1
]}

Kawamoto, H ^{[1
]}

Nishimura, T ^{[1
]}

Nishimura, I ^{[1
]}

Yoshinari, T ^{[1
]}

Arakawa, H ^{[1
]}

Suda, H ^{[1
]}

Morishima, H ^{[1
]}

Nishimura, S ^{[1
]}

机构：

[1] Merck Res Labs, Banyu Tsukuba Res Inst, Tsukuba, Ibaraki 3002611, Japan

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 1999年 / 9卷 / 09期

关键词：

anticancer agents; topoisomerase; indolocarbazole; substituent effects;

D O I：

10.1016/S0960-894X(99)00188-2

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

6-N-Amino analogues of NB-506 [6-N-formylamino-12,13-dihydro-1,11-dihydroxy-13-(beta-D-glucopyranosyl)-5H-indolo [2,3-a]pyrrolo[3,4-c]carbazole-5,7(6H)-dione] (3b) were synthesized and tested with respect to topoisomerase inhibition, cytotoxicity and anticancer effects. Among them, a 1,3-dihydroxypropane analogue (J-109,404, St) showed more than ten times more potent anticancer activity in MKN-45 human stomach cancer cells implanted in mice than NB-506. (C) 1999 Elsevier Science Ltd. All rights reserved.

引用

页码：1219 / 1224

页数：6

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