The preparation of ester heterocycles mostly uses heteroatoms as nucleophilic sites, which are achieved by intramolecular substitution or addition reactions. Compound: 3-Bromo-4-chloronitrobenzene( cas:16588-26-4 ) is researched.Application of 16588-26-4.Lucas, Simon C. C.; Atkinson, Stephen J.; Bamborough, Paul; Barnett, Heather; Chung, Chun-wa; Gordon, Laurie; Mitchell, Darren J.; Phillipou, Alexander; Prinjha, Rab K.; Sheppard, Robert J.; Tomkinson, Nicholas C. O.; Watson, Robert J.; Demont, Emmanuel H. published the article 《Optimization of Potent ATAD2 and CECR2 Bromodomain Inhibitors with an Atypical Binding Mode》 about this compound( cas:16588-26-4 ) in Journal of Medicinal Chemistry. Keywords: ATAD2 CECR2 inhibitor cat eye syndrome bromodomains. Let’s learn more about this compound (cas:16588-26-4).
Most bromodomain inhibitors mimic the interactions of the natural acetylated lysine (KAc) histone substrate through key interactions with conserved asparagine and tyrosine residues within the binding pocket. Herein we report the optimization of a series of Ph sulfonamides that exhibit a novel mode of binding to non-bromodomain and extra terminal domain (non-BET) bromodomains through displacement of a normally conserved network of four water mols. Starting from an initial hit mol., we report its divergent optimization toward the ATPase family AAA domain containing 2 (ATAD2) and cat eye syndrome chromosome region, candidate 2 (CECR2) domains. This work concludes with the identification of (R)-55 (GSK232)(I), a highly selective, cellularly penetrant CECR2 inhibitor with excellent physicochem. properties.
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