Structure–activity relationship study of acridine analogs as haspin and DYRK2 kinase inhibitors

…, NP Ulyanova, D Patnaik, V Pique, G Casano…

Index: Cuny, Gregory D.; Robin, Maxime; Ulyanova, Natalia P.; Patnaik, Debasis; Pique, Valerie; Casano, Gilles; Liu, Ji-Feng; Lin, Xiangjie; Xian, Jun; Glicksman, Marcie A.; Stein, Ross L.; Higgins, Jonathan M.G. Bioorganic and Medicinal Chemistry Letters, 2010 , vol. 20, # 12 p. 3491 - 3494

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Citation Number: 21

Abstract

Haspin is a serine/threonine kinase required for completion of normal mitosis that is highly expressed during cell proliferation, including in a number of neoplasms. Consequently, it has emerged as a potential therapeutic target in oncology. A high throughput screen of approximately 140,000 compounds identified an acridine analog as a potent haspin kinase inhibitor. Profiling against a panel of 270 kinases revealed that the compound also ...