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Synthesis and biological properties of benzo-annulated rutaecarpines
Young Hwan Hong1, Woo Jin Lee, Seung Ho Lee
1College of Pharmacy, Yeungnam University, Gyeongsan 712–749, Korea.
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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