Quality Control of 2-Hydroxyphenylboronic acidIn 2021 ,《Design and synthesis of 1H-pyrazolo[3,4-b]pyridines targeting mitogen-activated protein kinase kinase 4 (MKK4) – A promising target for liver regeneration》 appeared in European Journal of Medicinal Chemistry. The author of the article were Pfaffenrot, Bent; Kloevekorn, Philip; Juchum, Michael; Selig, Roland; Albrecht, Wolfgang; Zender, Lars; Laufer, Stefan A.. The article conveys some information:
Currently, the therapeutic options for treatment of liver failure are very limited. As mitogen-activated protein kinase kinase 4 (MKK4) has recently been identified by in vivo RNAi experiments to be a major regulator in hepatocyte regeneration, authors pursued the development of a small mol. targeting this protein kinase. Starting from the approved BRAFV600E inhibitor vemurafenib, that showed a high off-target affinity to MKK4 in an initial screening, authors followed a scaffold-hopping approach, changing the core heterocycle from 1H-pyrrolo[2,3-b]pyridine to 1H-pyrazolo[2,3-b]pyridine I. Affinity to MKK4 could be conserved while the selectivity against off-target protein kinases was slightly improved. Further modifications led to II and III showing high affinity to MKK4 in the low nanomolar range and excellent selectivity profile from mandatory multiparameter-optimization for the essential anti-targets (MKK7, JNK1) and off-targets (BRAF, MAP4K5, ZAK) in the MKK4 pathway. Herein authors report the first selective MKK4 inhibitors in this class. In the part of experimental materials, we found many familiar compounds, such as 2-Hydroxyphenylboronic acid(cas: 89466-08-0Quality Control of 2-Hydroxyphenylboronic acid)
2-Hydroxyphenylboronic acid(cas: 89466-08-0) belongs to acyl phenylboronic acid. Phenylboronic acid (PBA) has been used to extract β-blockers (a class of aminoalcohol-containing drugs) from aqueous solution, rat, and human plasma. Quality Control of 2-Hydroxyphenylboronic acid
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