Sulfamate Acetamides as Self-Immolative Electrophiles for Covalent Ligand-Directed Release Chemistry

Electrophiles for covalent inhibitors that are suitable for in vivo administration are rare. While acrylamides are prevalent in FDA-approved covalent drugs, chloroacetamides are considered too reactive for such purposes. We report sulfamate-based electrophiles that maintain chloroacetamide-like geom...

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Veröffentlicht in:	Journal of the American Chemical Society 2023-02, Vol.145 (6), p.3346-3360
Hauptverfasser:	Reddi, Rambabu N., Rogel, Adi, Gabizon, Ronen, Rawale, Dattatraya Gautam, Harish, Battu, Marom, Shir, Tivon, Barr, Arbel, Yamit Shorer, Gurwicz, Neta, Oren, Roni, David, Keren, Liu, Jingjing, Duberstein, Shirly, Itkin, Maxim, Malitsky, Sergey, Barr, Haim, Katz, Ben-Zion, Herishanu, Yair, Shachar, Idit, Shulman, Ziv, London, Nir
Format:	Artikel
Sprache:	eng
Schlagworte:	Acetamides Animals Ligands Mice Protein Kinase Inhibitors - pharmacology
Online-Zugang:	Volltext
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