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Design and biological evaluation of substituted 5,7-dihydro-6H-indolo[2,3-c]quinolin-6-one as novel selective Haspin inhibitors. 2022
Sreenivas Avula, and
Xudan Peng, and
Xingfen Lang, and
Micky Tortorella, and
Béatrice Josselin, and
Stéphane Bach, and
Stephane Bourg, and
Pascal Bonnet, and
Frédéric Buron, and
Sandrine Ruchaud, and
Sylvain Routier, and
Cleopatra Neagoie
Guangzhou Institute of Biomedicine and Health, Chinese Academy of Science, Guangzhou, China.
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.
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