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ID: ALA4020766
Journal: Bioorg Med Chem Lett
Title: Design and synthesis of potent inhibitors of the mono(ADP-ribosyl)transferase, PARP14.
Authors: Upton K, Meyers M, Thorsell AG, Karlberg T, Holechek J, Lease R, Schey G, Wolf E, Lucente A, Schüler H, Ferraris D.
Abstract: A series of (Z)-4-(3-carbamoylphenylamino)-4-oxobut-2-enyl amides were synthesized and tested for their ability to inhibit the mono-(ADP-ribosyl)transferase, PARP14 (a.k.a. BAL-2; ARTD-8). Two synthetic routes were established for this series and several compounds were identified as sub-micromolar inhibitors of PARP14, the most potent of which was compound 4t, IC50=160nM. Furthermore, profiling other members of this series identified compounds with >20-fold selectivity over PARP5a/TNKS1, and modest selectivity over PARP10, a closely related mono-(ADP-ribosyl)transferase.
CiteXplore: 28495083