Shubhendu
Palei
,
Jörn
Weisner
,
Melina
Vogt
,
Rajesh
Gontla
,
Benjamin
Buchmuller
,
Christiane
Ehrt
,
Tobias
Grabe
,
Silke
Kleinbölting
,
Matthias
Müller
,
Guido H.
Clever
*,
Daniel
Rauh
* and
Daniel
Summerer
*
Department of Chemistry and Chemical Biology, TU Dortmund University and, Drug Discovery Hub Dortmund (DDHD), Zentrum für Integrierte Wirkstoffforschung (ZIW), Otto-Hahn Str. 4a, 44227 Dortmund, Germany. E-mail: guido.clever@tu-dortmund.de; daniel.rauh@tu-dortmund.de; daniel.summerer@tu-dortmund.de
First published on 29th January 2024
Correction for ‘A high-throughput effector screen identifies a novel small molecule scaffold for inhibition of ten-eleven translocation dioxygenase 2’ by Shubhendu Palei et al., RSC Med. Chem., 2022, 13, 1540–1548, https://doi.org/10.1039/D2MD00186A.
The authors conducted additional SAR, revealing that the sulfonic acid group of 2 can replace the carboxyl group of IOX1, leading to a simple sulfonic acid-based quinoline 18 with a virtually identical IC50. In contrast, a replacement of IOX1's 8-hydroxyl group with a fluorine atom led to inactivity (19). The authors further identified and validated other IOX1-derived compounds without the 8HQ core that nevertheless showed micromolar IC50 values, such as isoquinoline-3-carboxylic acid (20), tetrahydroisoquinoline-6,7-diol (21), and 3-hydroxypicolinic acid (22). This combined data indicates that the 8HQ core is essential for hTET2 inhibition by IOX1 itself, whereas it is not essential for IOX1-derived compounds in general, providing new starting points for TET2 inhibitors without the 8HQ core.
An updated version of Table 1 is included here.
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