Lead change of a HIF-2α antagonist guided by multiparameter optimization and utilization of an Olp→π*Ar interaction-Reference-Cited by-同舟云学术

Lead change of a HIF-2α antagonist guided by multiparameter optimization and utilization of an Olp→π*Ar interaction

Published:2023-07 Issue:7 Volume:32 Page:1510-1531
ISSN:1054-2523
Container-title:Medicinal Chemistry Research
language:en
Short-container-title:Med Chem Res

Author:

Wehn Paul M.^ORCID,Yang Song^ORCID,Grina Jonas A.,Rizzi James P.,Schlachter Stephen T.,Wang Bin,Xu Rui,Yang Hanbiao,Du Xinlin,Han Guangzhou,Wang Keshi,Czerwinski Robert M.,Ged Emily L.,Huang Heli,Halfmann Megan M.,Maddie Melissa A.,Morton Emily R.,Olive Sarah R.,Tan Huiling,Xie Shanhai,Josey John A.,Wallace Eli M.

Publisher

Springer Science and Business Media LLC

Subject

Organic Chemistry,General Pharmacology, Toxicology and Pharmaceutics

Link

https://link.springer.com/content/pdf/10.1007/s00044-023-03088-w.pdf

Reference44 articles.

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4. Jaakkola P, Mole DR, Tian Y-M, Wilson MI, Gielbert J, Gaskell SJ, et al. Targeting of HIF-α to the von Hippel-Lindau ubiquitylation complex by O2 - regulated prolyl hydroxylation. Science. 2001;292:468–72. https://doi.org/10.1126/science.1059796.

5. Bruick RK, McKnight SL. A conserved family of Prolyl-4-hydroxylases that modify HIF. Science. 2001;294:1337–40. https://doi.org/10.1126/science.1066373.

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1. Recent progress in the development of hypoxia-inducible factor 2α (HIF-2α) modulators: Inhibitors, agonists, and degraders (2009–2024);European Journal of Medicinal Chemistry;2024-09

2. Synthesis of the Hypoxia-Inducible Factor-2α (HIF-2α) Inhibitor, 3-[(1S,2S,3R)-2,3-Difluoro-1-hydroxy-7-methylsulfonylindan-4-yl]oxy-5-fluorobenzonitrile (PT2977, Belzutifan); Efficient Replication of Established Approaches;Tetrahedron Letters;2023-09