Discovery of EEDi-5273 as an Exceptionally Potent and Orally Efficacious EED Inhibitor Capable of Achieving Complete and Persistent Tumor Regression.
Autor: | Rej RK, Wang C, Lu J, Wang M, Petrunak E, Zawacki KP, McEachern D, Yang CY; Department of Pharmaceutical Sciences, College of Pharmacy, University of Tennessee Health Science Center, Memphis, Tennessee 38163, United States., Wang L, Li R, Chinnaswamy K, Wen B, Sun D, Stuckey JA, Zhou Y; Ascentage Pharma Group, Suzhou, Jiangsu 215216, China., Chen J; Ascentage Pharma Group, Suzhou, Jiangsu 215216, China., Tang G; Ascentage Pharma Group, Suzhou, Jiangsu 215216, China., Wang S |
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Jazyk: | angličtina |
Zdroj: | Journal of medicinal chemistry [J Med Chem] 2021 Oct 14; Vol. 64 (19), pp. 14540-14556. Date of Electronic Publication: 2021 Oct 06. |
DOI: | 10.1021/acs.jmedchem.1c01059 |
Abstrakt: | Embryonic ectoderm development (EED) is a promising therapeutic target for human cancers and other diseases. We report herein the discovery of exceptionally potent and efficacious EED inhibitors. By conformational restriction of a previously reported EED inhibitor, we obtained a potent lead compound. Further optimization of the lead yielded exceptionally potent EED inhibitors. The best compound EEDi-5273 binds to EED with an IC |
Databáze: | MEDLINE |
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