Quality Control of 1-Benzyl-5-nitro-1H-indazole. Aromatic compounds can be divided into two categories: single heterocycles and fused heterocycles. Compound: 1-Benzyl-5-nitro-1H-indazole, is researched, Molecular C14H11N3O2, CAS is 23856-20-4, about Targeting Her2-insYVMA with Covalent Inhibitors-A Focused Compound Screening and Structure-Based Design Approach. Author is Lategahn, Jonas; Hardick, Julia; Grabe, Tobias; Niggenaber, Janina; Jeyakumar, Kirujan; Keul, Marina; Tumbrink, Hannah L.; Becker, Christian; Hodson, Luke; Kirschner, Tonia; Kloevekorn, Philip; Ketzer, Julia; Baumann, Matthias; Terheyden, Susanne; Unger, Anke; Weisner, Joern; Mueller, Matthias P.; van Otterlo, Willem A. L.; Bauer, Sebastian; Rauh, Daniel.
Mutated or amplified Her2 serves as a driver of non-small cell lung cancer or mediates resistance toward the inhibition of its family member epidermal growth factor receptor with small-mol. inhibitors. To date, small-mol. inhibitors targeting Her2 which can be used in clin. routine are lacking, and therefore, the development of novel inhibitors was undertaken. In this study, the well-established pyrrolopyrimidine scaffold was modified with structural motifs identified from a screening campaign with more than 1600 compounds, which were applied against wild-type Her2 and its mutant variant Her2-A775_G776insYVMA. The resulting inhibitors were designed to covalently target a reactive cysteine in the binding site of Her2 and were further optimized by means of structure-based drug design utilizing a set of obtained complex crystal structures. In addition, the anal. of binding kinetics and absorption, distribution, metabolism, and excretion parameters as well as mass spectrometry experiments and western blot anal. substantiated our approach.
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Highly efficient and robust molecular ruthenium catalysts for water oxidation,
Catalysts | Special Issue : Ruthenium Catalysts – MDPI