Machine-assisted synthesis of modulators of the histone reader BRD9 using flow methods of chemistry and frontal affinity chromatography

…, NA Burgess-Brown, CM Strain-Damerell…

Index: Guetzoyan, Lucie; Ingham, Richard J.; Nikbin, Nikzad; Rossignol, Julien; Wolling, Michael; Baumert, Mark; Burgess-Brown, Nicola A.; Strain-Damerell, Claire M.; Shrestha, Leela; Brennan, Paul E.; Fedorov, Oleg; Knapp, Stefan; Ley, Steven V. MedChemComm, 2014 , vol. 5, # 4 p. 540 - 546

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Citation Number: 13

Abstract

A combination of conventional organic synthesis, remotely monitored flow synthesis and bioassay platforms, were used for the evaluation of novel inhibitors targeting bromodomains outside the well-studied bromodomain and extra terminal (BET) family, here exemplified by activity measurements on the bromodomain of BRD9 protein, a component of some tissue- specific SWi/SNF chromatin remodelling complexes. The Frontal Affinity Chromatography ...