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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Detalhes bibliográficos
Publicado no:ACS Med Chem Lett
Main Authors: 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
Formato: Artigo
Idioma:Inglês
Publicado em: American Chemical Society 2016
Acesso em linha: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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