Previously employed non-selective protein kinase inhibitors yielded inconclusive results regarding involvement of protein kinase C (PKC) in phosphorylation of 47 kDa protein (p47 phox) in intact neutrophils stimulated with physiologic agonists of superoxide generation. In the present study, phos...

The involvement of protein kinase C (PKC) isoforms in glucose-induced insulin secretion was investigated by comparing the effects of the PKC inhibitors Gö 6976, which is PKC-specific and selective for the Ca2+-dependent isoforms, and Ro 31-8220, a specific PKC inhibitor which does not discrimina...

The bisindolylmaleimide Ro 31-8220 is a selective inhibitor of protein kinase C. This compound was used to investigate the involvement of protein kinase C in the stimulation of gastric acid secretion by the muscarinic cholinergic receptor on rat isolated parietal cells. The accumulation of the w...

The PKC-inhibitor Ro 31-8220 inhibits stimulated fluid pinocytosis of human PMNs induced by the PKC-activators phorbol myristate acetate (PMA, IC50 = 1.35×10−6M) or diacylglycerols (OAG, diC8) by 95%, whereas Ro 31-8220 has no effect on D2O- or fNLPNTL-induced pinocytosis and enhances cytochala...

Platelet-derived growth factor (PDGF) stimulates the hydrolysis of phosphatidylinositol 4,5-bisphosphate (Ptd InsP2) via phospholipase C-γ1 (PLC-γ1) in Swiss 3T3 cells. Treatment of cells with the protein kinase C (PKC) inhibitor Ro-31-8220 greatly decreased PDGF-induced tyrosine phosphorylati...

SummaryTwo new potent protein kinase C inhibitors, RO 31-8220 and RO 31-7549, and staurosporine were found to inhibit dose-dependently the phorbol ester-induced formation of prostaglandin E2and superoxide in cultured liver macrophages. Prostaglandin E2formation from exogenously added arachidonat...

RO 31-8220 is a bisindolemaleimide derivative of …

The intraneuronal aggregates of hyperphosphorylated and misfolded tau (neurofibrillary tangles, NFTs) cause a stereotypical spatiotemporal Alzheimer's disease (AD) progression that correlates with the severity of the associated cognitive decline. Kinase activity contributes to the balance b...

The novel bisphosphonate (BP) disodium dihydrogen-4-[(methylthio) phenylthio] methanebisphosphonate (MPMBP) is a non-nitrogen-containing BP with an antioxidant side chain that possesses anti-inflammatory properties. We investigated the systemic effects of this compound on bone loss induced by ov...

To overcome the drug-resistance of first generation EGFR inhibitors and the nonselective toxicities of second generation inhibitors among NSCLC patients, a series of 5-(methylthio)pyrimidine derivatives were discovered as novel EGFR inhibitors, which harbored not only potent enzymatic and antipr...

Reaction of [Ru(PPh3)3Cl2] with 2-(methylthio)phenylsalicylaldimine Schiff-base (HL) in tetrahydrofuran (THF) in the presence of triethylamine afforded a ruthenium(II) complex [Ru(ONS-L)(PPh3)2Cl]·CH3OH·2.75H2O (1). Similarly, reaction of [Ru(CO)2Cl2] with HL in N,N′-dimethylformamide (DMF) i...

A practical modification of the Gassman 3-(methylthio)oxindole synthesis is reported. In our method, substituted anilines and 2-(methylthio)acetamide were reacted under mild reaction conditions, in the presence of N-chlorophthalimide as a chlorinating agent to give α-amidosulfides, which, in th...

An organocatalytic asymmetric [3 + 2] cycloaddition of trifluoromethyl-containing azomethine ylides with cyclic 2,4-dienones was developed. The process enables efficient incorporation of CF3 groups into functionalized spiro[pyrrolidin-3,2′-oxindoles] in high yields with good to excellent enanti...

Herein, we describe the preparation of trifluoromethylthiol-substituted oxindoles by silver-mediated aryltrifluoromethylthiolation of activated alkenes, using S-trifluoromethyl 4-methylbenzenesulfonothioate as a F3CS radical source and showing that the reagent availability, mild conditions, and ...

The transition metal complexes are playing the crucial role in advancement of modern chemical science. In the present study, we synthesized the Pd(II) complex [Pd2 (C5H5F3N2)2(C5H4F3N2)2Cl2]·3(C2H6O), 1 with 3-Methyl-5-(trifluoromethyl) pyrazole ligand. The complex 1 has been characterized by I...

We have achieved an efficient synthesis of 1,1-dimethyl-3-(trifluoromethyl)-1H-isoindole N-oxide (2) in 39% yield by seven steps from 2-bromobenzoic acid (3). This compound serves as a spin trap reagent, giving a strong and stable ESR signal of the radical adduct of 2 in the presence of i-amylox...

The ferric chloride-promoted direct trifluoromethylselenolation of indoles and other nitrogen-containing heterocyclic compounds in water was performed by employing TsSeCF3 as a trifluoromethylselenolation reagent. The shelf-stable and readily accessible reagents, along with the environmentally f...

A hexapeptide containing a β-d-Galp-(1 → 3)-α-d-Galp NAc-(1 → O)-l-threonine unit was synthesized using glycosylated pentafluorophenyl esters in an Fmoc-based strategy. In all of the glycosylation reactions, trichloroacetimidates were successfully employed. The disaccharide moiety was prepar...

An octasaccharide, β-d-Galp-(1 → 6)-[α-l-Araf-(1 → 2)]-β-d-Galp-(1 → 6)-β-d-Galp-(1 → 6)-[α-l-Araf-(1 → 5)-α-l-Araf-(1 → 2)]-β-d-Galp-(1 → 6)-β-d-Galp-1 → OMP was synthesized. 4-Methoxyphenyl 2,3,4-tri-O-benzoyl-β-d-galactopyranoside (5), 2,6-di-O-acetyl-3,4-di-O-benzoyl-α-d-ga...

A novel series of 3-(1-(1-substituted piperidin-4-yl)-1H-1,2,3-triazol-4-yl)-5-substituted phenyl-1,2,4-oxadiazoles bearing 1,2,3-triazole and piperidine ring has been synthesized in one step from amidoxime using Carbonyl diimidazole (CDI) and K2CO3. All the synthesized compounds (4a–4r) are no...