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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Publicat a:ACS Med Chem Lett
Autors principals: 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
Format: Artigo
Idioma:Inglês
Publicat: American Chemical Society 2021
Accés en línia: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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