Design and synthesis of potent inhibitors of the mono(ADP-ribosyl)transferase, PARP14
Upton, Kristen ; Meyers, Matthew ; Thorsell, Ann-Gerd ; Karlberg, Tobias LU ; Holechek, Jacob ; Lease, Robert ; Schey, Garrett ; Wolf, Emily ; Lucente, Adrianna and Schüler, Herwig LU
, et al.
(2017)
In Bioorganic & Medicinal Chemistry Letters
27(13).
p.2907-2911
- 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.
Please use this url to cite or link to this publication:
https://lup.lub.lu.se/record/a5467934-a5b3-429a-bd72-8344cf6832c2
- author
- Upton, Kristen
; Meyers, Matthew
; Thorsell, Ann-Gerd
; Karlberg, Tobias
LU
; Holechek, Jacob
; Lease, Robert
; Schey, Garrett
; Wolf, Emily
; Lucente, Adrianna
and Schüler, Herwig
LU
, et al. (More)
- Upton, Kristen
; Meyers, Matthew
; Thorsell, Ann-Gerd
; Karlberg, Tobias
LU
; Holechek, Jacob
; Lease, Robert
; Schey, Garrett
; Wolf, Emily
; Lucente, Adrianna
; Schüler, Herwig
LU
and Ferraris, Dana
(Less)
- publishing date
- 2017-07-01
- type
- Contribution to journal
- publication status
- published
- keywords
- Dose-Response Relationship, Drug, Drug Design, Humans, Models, Molecular, Molecular Structure, Poly(ADP-ribose) Polymerase Inhibitors/chemistry, Poly(ADP-ribose) Polymerases/metabolism, Structure-Activity Relationship
- in
- Bioorganic & Medicinal Chemistry Letters
- volume
- 27
- issue
- 13
- pages
- 5 pages
- publisher
- Elsevier
- external identifiers
-
- pmid:28495083
- scopus:85019026432
- ISSN
- 0960-894X
- DOI
- 10.1016/j.bmcl.2017.04.089
- language
- English
- LU publication?
- no
- additional info
- Copyright © 2017 Elsevier Ltd. All rights reserved.
- id
- a5467934-a5b3-429a-bd72-8344cf6832c2
- date added to LUP
- 2024-11-21 17:51:07
- date last changed
- 2025-05-09 22:31:19
@article{a5467934-a5b3-429a-bd72-8344cf6832c2,
abstract = {{<p>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.</p>}},
author = {{Upton, Kristen and Meyers, Matthew and Thorsell, Ann-Gerd and Karlberg, Tobias and Holechek, Jacob and Lease, Robert and Schey, Garrett and Wolf, Emily and Lucente, Adrianna and Schüler, Herwig and Ferraris, Dana}},
issn = {{0960-894X}},
keywords = {{Dose-Response Relationship, Drug; Drug Design; Humans; Models, Molecular; Molecular Structure; Poly(ADP-ribose) Polymerase Inhibitors/chemistry; Poly(ADP-ribose) Polymerases/metabolism; Structure-Activity Relationship}},
language = {{eng}},
month = {{07}},
number = {{13}},
pages = {{2907--2911}},
publisher = {{Elsevier}},
series = {{Bioorganic & Medicinal Chemistry Letters}},
title = {{Design and synthesis of potent inhibitors of the mono(ADP-ribosyl)transferase, PARP14}},
url = {{http://dx.doi.org/10.1016/j.bmcl.2017.04.089}},
doi = {{10.1016/j.bmcl.2017.04.089}},
volume = {{27}},
year = {{2017}},
}