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Biological and Pharmaceutical Bulletin
Online ISSN : 1347-5215
Print ISSN : 0918-6158
ISSN-L : 0918-6158
Regular Articles
Synthesis and Biological Properties of Benzo-Annulated Rutaecarpines
Young Hwan Hong, Woo Jin Lee, Seung Ho Lee, Jong Keun Son, Hye-Lin Kim, Jung Min Nam, Youngjoo Kwon, Yurngdong Jahng
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Keywords: rutaecarpine, benzorutaecarpine, Fischer indole synthesis, topoisomerase, cytotoxicity
JOURNAL FREE ACCESS

2010 Volume 33 Issue 10 Pages 1704-1709

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Abstract

A series of benzo-annulated rutaecarpines were prepared from anthranilic acid and 3-aminonaphthalene-2-carboxylic acid by Fischer indole synthesis as key reaction. Cytotoxicity was somewhat increased by the introduction of benzo-annulation, which was not directly related to the inhibitory activity against topoisomerases (topo) I and II. Benzo-annulation on ring A led to significant increase of inhibitory activity against topo II while annulations on ring E increased inhibitory activity against topo I.

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© 2010 The Pharmaceutical Society of Japan
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