Pyrazoles are synthesized by the reaction of α,β-unsaturated aldehydes with hydrazine and subsequent dehydrogenation. 269410-08-4, formula is C9H15BN2O2, Name is 4-(4,4,5,5-Tetramethyl-1,3,2-dioxaborolan-2-yl)-1H-pyrazole. Substituted pyrazoles are prepared by condensation of 1,3-diketones with hydrazine (Knorr-type reactions). For example, acetylacetone and hydrazine gives 3,5-dimethylpyrazole. SDS of cas: 269410-08-4.
Gilles, Philippe;Kashyap, Rudra S.;Freitas, Maria Joao;Ceusters, Sam;Van Asch, Koen;Janssens, Anke;De Jonghe, Steven;Persoons, Leentje;Cobbaut, Mathias;Daelemans, Dirk;Van Lint, Johan;Voet, Arnout R. D.;De Borggraeve, Wim M. research published 《 Design, synthesis and biological evaluation of pyrazolo[3,4-d]pyrimidine-based protein kinase D inhibitors》, the research content is summarized as follows. Novel pyrazolo[3,4-d]pyrimidine based pan-PKD inhibitors I [R1 = tBu, 3,3-dimethylbutyl, Bn, etc.; R2 = pyrrol-3-yl, indol-3-yl, naphthalen-1-yl, etc.] with structural variety at position 1 were synthesized and evaluated for biol. activity. Compounds I were evaluated for PKD inhibition against full length PKD using Promega’s ADP-GloTM kinase activity assay and syntide-2 as a substrate. Starting from compound I [R1 = tBu; R2 = indol-3-yl] a known PKD inhibitor with IC50 values in the range of 94-108 nM, compound I [R1 = (piperidin-4-yl)methyl; R2 = indol-3-yl] was identified with an improved biochem. inhibitory activity against PKD (IC50 = 17-35 nM). Subsequent cellular assays demonstrated that compounds I [R1 = tBu, (piperidin-4-yl)methyl; R2 = indol-3-yl] inhibited PKD-dependent cortactin phosphorylation. Furthermore, the biochem. inhibitory activity of I [R1 = tBu; R2 = indol-3-yl] and 1-NM-PP1 against CAMKIIα and PKCδ was investigated and no notable inhibition was observed at compound concentrations of 1 and 10μM. Some of the synthesized PKD inhibitor compounds I [R1 = tBu, (piperidin-4-yl)methyl, 2,2-dimethyl-propan-1-ol, (1-Me-piperidin-4-yl)methyl; R2 = indol-3-yl, 1-Me-indol-3-yl, 2-ethoxyquinolin-6-yl] and some known PKD inhibitors (CRT0066101, 1-NM-PP1) were evaluated for their antitumor activity in a panel of eight different cancer cell lines. A screening against different cancer cell lines demonstrated that compound I [R1 = tBu; R2 = indol-3-yl] was potent and versatile antitumoral agent.
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., SDS of cas: 269410-08-4
Referemce:
Pyrazole – Wikipedia,
Pyrazoles – an overview | ScienceDirect Topics