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. 2017 Jul 1;27(13):2907-2911.
doi: 10.1016/j.bmcl.2017.04.089. Epub 2017 Apr 29.

Design and synthesis of potent inhibitors of the mono(ADP-ribosyl)transferase, PARP14

Kristen Upton  1 , Matthew Meyers  1 , Ann-Gerd Thorsell  2 , Tobias Karlberg  2 , Jacob Holechek  1 , Robert Lease  1 , Garrett Schey  1 , Emily Wolf  3 , Adrianna Lucente  3 , Herwig Schüler  2 , Dana Ferraris  4
Affiliations

Design and synthesis of potent inhibitors of the mono(ADP-ribosyl)transferase, PARP14

Kristen Upton et al. Bioorg Med Chem Lett. .

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.

Keywords: ARTD-8; Mono(ADP-ribosyl) transferase; PARP; PARP14.

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