The discovery of tetrahydro-β-carbolines as inhibitors of the kinesin Eg5

…, N Brammeier, E Martin, D Bussiere, AO Walter

Index: Barsanti, Paul A.; Wang, Weibo; Ni, Zhi-Jie; Duhl, David; Brammeier, Nathan; Martin, Eric; Bussiere, Dirksen; Walter, Annette O. Bioorganic and Medicinal Chemistry Letters, 2010 , vol. 20, # 1 p. 157 - 160

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Citation Number: 54

Abstract

A series of tetrahydro-β-carbolines were identified by HTS as inhibitors of the kinesin Eg5. Molecular modeling and medicinal chemistry techniques were employed to explore the SAR for this series with a focus of removing potential metabolic liabilities and improving cellular potency.