%0 Journal Article %T Design and biological evaluation of substituted 5,7-dihydro-6 H -indolo[2,3- c ]quinolin-6-one as novel selective Haspin inhibitors %+ Guangzhou Institute of Biomedicine and Health %+ Laboratoire de Biologie Intégrative des Modèles Marins (LBI2M) %+ Station biologique de Roscoff (SBR) %+ Fédération de recherche de Roscoff (FR2424) %+ Institut de Chimie Organique et Analytique (ICOA) %A Avula, Sreenivas %A Peng, Xudan %A Lang, Xingfen %A Tortorella, Micky %A Josselin, Béatrice %A Bach, Stéphane %A Bourg, Stephane %A Bonnet, Pascal %A Buron, Frédéric %A Ruchaud, Sandrine %A Routier, Sylvain %A Neagoie, Cleopatra %< avec comité de lecture %@ 1475-6366 %J Journal of Enzyme Inhibition and Medicinal Chemistry %I Informa Healthcare %V 37 %N 1 %P 1632-1650 %8 2022 %D 2022 %R 10.1080/14756366.2022.2082419 %K Indoloquinoline %K Haspin kinase %K docking %K cell viability %Z Chemical Sciences/Medicinal ChemistryJournal articles %X A library of substituted indolo[2,3-c]quinolone-6-ones was developed as simplified Lamellarin isosters. Synthesis was achieved from indole after a four-step pathway sequence involving iodination, a Suzuki-Miyaura cross-coupling reaction, and a reduction/lactamization sequence. The inhibitory activity of the 22 novel derivatives was assessed on Haspin kinase. Two of them possessed an IC50 of 1 and 2 nM with selectivity towards a panel of 10 other kinases including the parent kinases DYRK1A and CLK1. The most selective compound exerted additionally a very interesting cell effect on the osteosarcoma U-2 OS cell line. %G English %2 https://hal.science/hal-03818922/document %2 https://hal.science/hal-03818922/file/Design%20and%20biological%20evaluation%20of%20substituted%205%207%20dihydro%206H%20indolo%202%203%20c%20quinolin%206%20one%20as%20novel%20selective%20Haspin%20inhibitors.pdf %L hal-03818922 %U https://hal.science/hal-03818922 %~ CEA %~ CNRS %~ UNIV-ORLEANS %~ ICOA %~ LBI2M %~ INC-CNRS %~ SORBONNE-UNIVERSITE %~ SORBONNE-UNIV %~ SU-SCIENCES %~ FR2424 %~ SU-TI %~ ALLIANCE-SU %~ TEST2-HALCNRS %~ TEST3-HALCNRS %~ SBR %~ LABOS-SYNORG