Discovery of Orally Bioavailable Ligand Efficient Quinazolindiones as Potent and Selective Tankyrases Inhibitors

[Image: see text] We report herein the discovery of quinazolindiones as potent and selective tankyrase inhibitors. Elucidation of the structure–activity relationship of the lead compound 1g led to truncated analogues that have good potency in cells, pharmacokinetic (PK) properties, and excellent sel...

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Detalhes bibliográficos
Publicado no:ACS Med Chem Lett
Main Authors: Qin, Donghui, Lin, Xiaojuan, Liu, Zhi, Chen, Yan, Zhang, Zhiliu, Wu, Chengde, Liu, Linlin, Pan, Yan, Laquerre, Sylvie, Emery, John, Fergusson, Jeff, Roland, Kimberly, Keenan, Rick, Oliff, Allen, Kumar, Sanjay, Cheung, Mui, Su, Dai-Shi
Formato: Artigo
Idioma:Inglês
Publicado em: American Chemical Society 2021
Acesso em linha:https://ncbi.nlm.nih.gov/pmc/articles/PMC8201761/
https://ncbi.nlm.nih.gov/pubmed/34141085
https://ncbi.nlm.nih.govhttp://dx.doi.org/10.1021/acsmedchemlett.1c00160
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