Synthesis and biological evaluation of Haspin inhibitors: Kinase inhibitory potency and cellular activity

We describe the structure-activity relationship study including the evaluation of this inhibitor on a large panel of 486 kinases as well as on immortalized or cancer cell lines. In addition, we determined the binding mode of analog 2a in complex with Haspin using X-ray crystallography.PMID:35447555 | DOI:10.1016/j.ejmech.2022.114369

Source: European Journal of Medicinal Chemistry - April 21, 2022 Category: Chemistry Authors: Wael Zeinyeh Yannick J Esvan B éatrice Josselin Mathilde Defois Blandine Baratte Stefan Knapp Apirat Chaikuad Fabrice Anizon Francis Giraud Sandrine Ruchaud Pascale Moreau Source Type: research