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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Publicat a:ACS Med Chem Lett
Autors principals: 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
Idioma:Inglês
Publicat: American Chemical Society 2016
Accés en línia: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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