期刊
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
卷 27, 期 13, 页码 2907-2911出版社
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmcl.2017.04.089
关键词
PARP; PARP14; ARTD-8; Mono(ADP-ribosyl) transferase
资金
- Swedish Cancer Society [2014/716]
- Swedish Research Council [201504603]
- IngaBritt and Arne Lundbergs Research Foundation [403]
- European Community's Seventh Framework Programme (FP7) under BioStruct-X [283570]
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 = 160 nM. 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. (C) 2017 Elsevier Ltd. All rights reserved.
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