Pyrazoles and pyrimidines have diverse biological and pharmacological activities. 269410-08-4, formula is C9H15BN2O2, Name is 4-(4,4,5,5-Tetramethyl-1,3,2-dioxaborolan-2-yl)-1H-pyrazole. There are a number of antimicrobial compounds containing pyrazole moiety as the core unit. Application of C9H15BN2O2.
Powell, Chelsea E.;Hatcher, John M.;Jiang, Jie;Vatsan, Prasanna S.;Che, Jianwei;Gray, Nathanael S. research published 《 Selective Macrocyclic Inhibitors of DYRK1A/B》, the research content is summarized as follows. Dual-specificity tyrosine-(Y)-phosphorylation regulated kinase 1A (DYRK1A) is a therapeutic target of interest due to the roles it plays in both neurol. diseases and cancer. We present the development of the first macrocyclic inhibitors of DYRK1A. Initial lead inhibitor JH-XIV-68-3 (3) displayed selectivity for DYRK1A and close family member DYRK1B in biochem. and cellular assays, and demonstrated antitumor efficacy in head and neck squamous cell carcinoma (HNSCC) cell lines. However, we noted that it suffered from rapid aldehyde oxidase (AO)-mediated metabolism To overcome this liability, we generated a derivative (JH-XVII-10 (10)), where fluorine was introduced to block the 2-position of the azaindole and render the mol. resistant to AO activity. We showed that 10 maintains remarkable potency and selectivity in biochem. and cellular assays as well as antitumor efficacy in HNSCC cell lines and improved metabolic stability. Therefore, 10 represents a promising new scaffold for developing DYRK1A-targeting chem. probes and therapeutics.
269410-08-4, 4-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)-1H-pyrazole, also known as 4-Pyrazoleboronic acid pinacol ester , is a useful research compound. Its molecular formula is C9H15BN2O2 and its molecular weight is 194.04 g/mol. The purity is usually 95%.
4-Pyrazoleboronic acid pinacol ester is a useful reagent for Suzuki-Miyaura cross-couplings as well as Ruthenium-catalyzed asymmetric hydrogenation. 4-Pyrazoleboronic acid pinacol ester is also a useful reagent for preparing VEGF, Aurora, RHO (ROCK), Janus Kinase 2, c-MET, ALK, S-nitrsoflutathione reductase, CDC7, Acetyl-CoA carboxylase inhibitors.
4-Pyrazoleboronic acid pinacol ester is used in the preparation of Rho kinase (ROCK) inhibitors as wella s other biologically active compounds.
4-Pyrazoleboronic acid pinacol ester is an organic compound that is the product of a bifunctional coupling reaction between 4-pyrazolecarboxylic acid and pinacol. It has been shown to inhibit protein S6 kinase, which is involved in the regulation of cell growth and proliferation. This compound has also been shown to be effective against cancer cells, including those that are resistant to conventional chemotherapeutic drugs. 4-Pyrazoleboronic acid pinacol ester may also be used as a precursor for other compounds with pharmaceutical activity., Application of C9H15BN2O2
Referemce:
Pyrazole – Wikipedia,
Pyrazoles – an overview | ScienceDirect Topics