Pyrazole is an organic compound with the formula C3H3N2H. It is a heterocycle characterized by a 5-membered ring of three carbon atoms and two adjacent nitrogen atoms, which are in ortho-substitution. 269410-08-4, formula is C9H15BN2O2, Name is 4-(4,4,5,5-Tetramethyl-1,3,2-dioxaborolan-2-yl)-1H-pyrazole. Pyrazoles are a class of compounds that have the ring C3N2 with adjacent nitrogen atoms.Notable drugs containing a pyrazole ring are celecoxib (celebrex) and the anabolic steroid stanozolol. Synthetic Route of 269410-08-4.
Vazquez-Rodriguez, Saleta;Wright, Miranda;Rogers, Catherine M.;Cribbs, Adam P.;Velupillai, Srikannathasan;Philpott, Martin;Lee, Henry;Dunford, James E.;Huber, Kilian V. M.;Robers, Matthew B.;Vasta, James D.;Thezenas, Marie-Laetitia;Bonham, Sarah;Kessler, Benedikt;Bennett, James;Fedorov, Oleg;Raynaud, Florence;Donovan, Adam;Blagg, Julian;Bavetsias, Vassilios;Oppermann, Udo;Bountra, Chas;Kawamura, Akane;Brennan, Paul E. research published 《 Design, Synthesis and Characterization of Covalent KDM5 Inhibitors》, the research content is summarized as follows. Histone lysine demethylases (KDMs) are involved in the dynamic regulation of gene expression and they play a critical role in several biol. processes. Achieving selectivity over the different KDMs has been a major challenge for KDM inhibitor development. Here we report potent and selective KDM5 covalent inhibitors designed to target cysteine residues only present in the KDM5 sub-family. The covalent binding to the targeted proteins was confirmed by MS and time-dependent inhibition. Addnl. competition assays show that compounds were non 2-OG competitive. Target engagement and ChIP-seq anal. showed that the compounds inhibited the KDM5 members in cells at nano- to micromolar levels and induce a global increase of the H3K4me3 mark at transcriptional start sites.
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., Synthetic Route of 269410-08-4
Referemce:
Pyrazole – Wikipedia,
Pyrazoles – an overview | ScienceDirect Topics