Synthesis of chromeno [3, 4-b] indoles as Lamellarin D analogues: A novel DYRK1A inhibitor class

…, O Lozach, L Meijer, B Baldeyrou, A Lansiaux…

Index: Neagoie, Cleopatra; Vedrenne, Emeline; Buron, Frederic; Merour, Jean-Yves; Rosca, Sorin; Bourg, Stephane; Lozach, Olivier; Meijer, Laurent; Baldeyrou, Brigitte; Lansiaux, Amelie; Routier, Sylvain European Journal of Medicinal Chemistry, 2012 , vol. 49, p. 379 - 396

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Citation Number: 36

Abstract

A library of substituted chromeno [3, 4-b] indoles was developed as Lamellarin isosters. Synthesis was achieved from indoles after a four-step pathway sequence involving C-3 iodination, a Suzuki cross-coupling reaction, and a one pot deprotection/lactonisation step. Twenty final compounds were tested in order to determine their activity against topoisomerase I and kinases, the two major biological activities of Lamellarins. One newly ...