2,8-Disubstituted-1,6-Naphthyridines and 4,6-Disubstituted-Isoquinolines with Potent, Selective Affinity for CDK8/19

[Image: see text] We demonstrate a designed scaffold-hop approach to the discovery of 2,8-disubstituted-1,6-naphthyridine- and 4,6-disubstituted-isoquinoline-based dual CDK8/19 ligands. Optimized compounds in both series exhibited rapid aldehyde oxidase-mediated metabolism, which could be abrogated...

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Veröffentlicht in:ACS Med Chem Lett
Hauptverfasser: Mallinger, Aurélie, Schiemann, Kai, Rink, Christian, Sejberg, Jimmy, Honey, Mark A., Czodrowski, Paul, Stubbs, Mark, Poeschke, Oliver, Busch, Michael, Schneider, Richard, Schwarz, Daniel, Musil, Djordje, Burke, Rosemary, Urbahns, Klaus, Workman, Paul, Wienke, Dirk, Clarke, Paul A., Raynaud, Florence I., Eccles, Suzanne A., Esdar, Christina, Rohdich, Felix, Blagg, Julian
Format: Artigo
Sprache:Inglês
Veröffentlicht: American Chemical Society 2016
Online Zugang:https://ncbi.nlm.nih.gov/pmc/articles/PMC4904262/
https://ncbi.nlm.nih.gov/pubmed/27326329
https://ncbi.nlm.nih.govhttp://dx.doi.org/10.1021/acsmedchemlett.6b00022
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