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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Veröffentlicht in:ACS Med Chem Lett
Hauptverfasser: 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
Sprache:Inglês
Veröffentlicht: American Chemical Society 2021
Online Zugang: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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