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Design and synthesis of potent inhibitors of the mono(ADP-ribosyl)transferase, PARP14. 2017
Kristen Upton, and
Matthew Meyers, and
Ann-Gerd Thorsell, and
Tobias Karlberg, and
Jacob Holechek, and
Robert Lease, and
Garrett Schey, and
Emily Wolf, and
Adrianna Lucente, and
Herwig Schüler, and
Dana Ferraris
McDaniel College, 2 College Hill, Westminster, MD 21157, United States.
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.
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