Bioorganic & medicinal chemistry letters

Aza-analogues of the marine pyrroloquinoline alkaloids wakayin and tsitsikammamines: synthesis and topoisomerase inhibition

L Legentil, B Lesur, E Delfourne

Index: Legentil, Laurent; Lesur, Brigitte; Delfourne, Evelyne Bioorganic and Medicinal Chemistry Letters, 2006 , vol. 16, # 2 p. 427 - 429

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Citation Number: 33

Abstract

Two aza-analogues of the marine pyrroloquinoline alkaloids wakayin and tsitsikammamines A and B have been synthesized. The strategy used was based on a 1, 3-dipolar cycloaddition reaction between indole 4, 7-dione and a diazo-aminopropane derivative. One of the two analogues partially inhibits human topoisomerase I, whereas synthetic intermediates inhibit the enzyme DNA cleavage activity at a concentration comparable to ...