4-Amino derivatives of the Hsp90 inhibitor CCT018159

…, A Massey, A Surgenor, J Wayne, P Workman…

Index: Barril, Xavier; Beswick, Mandy C.; Collier, Adam; Drysdale, Martin J.; Dymock, Brian W.; Fink, Alexandra; Grant, Kate; Howes, Robert; Jordan, Allan M.; Massey, Andrew; Surgenor, Allan; Wayne, Joanne; Workman, Paul; Wright, Lisa Bioorganic and Medicinal Chemistry Letters, 2006 , vol. 16, # 9 p. 2543 - 2548

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Citation Number: 88

Abstract

Novel piperazinyl, morpholino and piperidyl derivatives of the pyrazole-based Hsp90 inhibitor CCT018159 are described. Structure–activity relationships have been elucidated by X-ray co-crystal analysis of the new compounds bound to the N-terminal domain of human Hsp90. Key features of the binding mode are essentially identical to the recently reported potent analogue VER-49009. The most potent of the new compounds has a ...