Chemical probes to study ADP-ribosylation: synthesis and biochemical evaluation of inhibitors of the human ADP-ribosyltransferase ARTD3/PARP3

…, A Linusson, H Schüler, M Elofsson

文献索引：Lindgren, Anders E.G.; Karlberg, Tobias; Ekblad, Torun; Spjut, Sara; Thorsell, Ann-Gerd; Andersson, C. David; Nhan, Ton Tong; Hellsten, Victor; Weigelt, Johan; Linusson, Anna; Schueler, Herwig; Elofsson, Mikael Journal of Medicinal Chemistry, 2013 , vol. 56, # 23 p. 9556 - 9568

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被引用次数: 5

摘要

The racemic 3-(4-oxo-3, 4-dihydroquinazolin-2-yl)-N-[1-(pyridin-2-yl) ethyl] propanamide, 1, has previously been identified as a potent but unselective inhibitor of diphtheria toxin-like ADP-ribosyltransferase 3 (ARTD3). Herein we describe synthesis and evaluation of 55 compounds in this class. It was found that the stereochemistry is of great importance for both selectivity and potency and that substituents on the phenyl ring resulted in poor solubility. ...