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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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| Pubblicato in: | ACS Med Chem Lett |
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| Autori principali: | , , , , , , , , , , , , , , , , , , , , , |
| Natura: | Artigo |
| Lingua: | Inglês |
| Pubblicazione: |
American Chemical Society
2016
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| Accesso online: | 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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