Machine-assisted synthesis of modulators of the histone reader BRD9 using flow methods of chemistry and frontal affinity chromatographyElectronic supplementary information (ESI) available: Synthetic procedures, characterisation of prepared compounds, details of the set-up for frontal affinity chromatography, thermal shift assays data against 9 bromodomains. See DOI: 10.1039/c4md00007b

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 br...

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Main Authors: 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
Format: Article
Language:English
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Summary: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 combined with Mass Spectrometry (FAC-MS) method proved to be reliable and results correlated well with an independent thermal shift assay. Novel technologies were developed and used for the synthesis and evaluation of new triazolopyridazine BRD9 inhibitors.
ISSN:2040-2503
2040-2511
DOI:10.1039/c4md00007b