Synthesis of benz[d]indeno[1,2-b]pyran-5,11-diones:: Versatile intermediates for the design and synthesis of topoisomerase I inhibitors

被引：52

作者：

Morrell, A

Antony, S

Kohlhagen, G

Pommier, Y

Cushman, M ^{[1
]}

机构：

[1] Purdue Univ, Sch Pharm & Pharmaceut Sci, Dept Med Chem & Mol Pharmacol, W Lafayette, IN 47907 USA

[2] NCI, Mol Pharmacol Lab, Ctr Canc Res, Bethesda, MD 20892 USA

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2006年 / 16卷 / 07期

关键词：

indenoisoquinoline; topoisomerase I inhibitor; synthesis; anticancer;

D O I：

10.1016/j.bmcl.2006.01.008

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

A method has been developed that relies on a two-step, one-pot condensation between phthalide and 2-carboxybenzaldehydes to provide benz[a]indeno[ 1,2-h]pyran-5,11-diones in a multi-gram fashion. Treatment of these compounds with a primary amine allows rapid access to various N-substituted indenoisoquinolines, whose in vitro anticancer activity and topoisomerase I inhibition have been evaluated. (C) 2006 Elsevier Ltd. All rights reserved.

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页码：1846 / 1849

页数：4

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