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Synthesis and topoisomerase I inhibitory activity of a novel diazaindeno[2,1-b]phenanthrene analogue of Lamellarin D
Authors:Cananzi Salvatore  Merlini Lucio  Artali Roberto  Beretta Giovanni Luca  Zaffaroni Nadia  Dallavalle Sabrina
Affiliation:Department of Molecular and Agrifood Sciences, Università di Milano, Via Celoria 2, 20133 Milano, Italy.
Abstract:A novel 5-oxa-6a,8-diazaindeno[2,1-b]phenanthren-7-one scaffold was designed and synthesized as an active analogue of the cytotoxic marine alkaloid Lamellarin D. The design was based on molecular modeling of the site of interaction of Lamellarin D with DNA-topoisomerase I cleavable complex, whereas the synthesis capitalized on a simple Friedel-Crafts cyclization of indole to a β-carbolinone nucleus. The product exhibited topoisomerase I poisoning activity and submicromolar cytotoxicity on human non-small cell lung cancer H460 cell line.
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