Structure–activity relationship study of beta-carboline derivatives as haspin kinase inhibitors

GD Cuny, NP Ulyanova, D Patnaik, JF Liu, X Lin…

Index: Cuny, Gregory D.; Ulyanova, Natalia P.; Patnaik, Debasis; Liu, Ji-Feng; Lin, Xiangjie; Auerbach, Ken; Ray, Soumya S.; Xian, Jun; Glicksman, Marcie A.; Stein, Ross L.; Higgins, Jonathan M.G. Bioorganic and Medicinal Chemistry Letters, 2012 , vol. 22, # 5 p. 2015 - 2019

Full Text: HTML

Citation Number: 21

Abstract

Haspin is a serine/threonine kinase that phosphorylates Thr-3 of histone H3 in mitosis that has emerged as a possible cancer therapeutic target. High throughput screening of approximately 140,000 compounds identified the beta-carbolines harmine and harmol as moderately potent haspin kinase inhibitors. Based on information obtained from a structure– activity relationship study previously conducted for an acridine series of haspin inhibitors ...