Search results for "pyridines"
showing 10 items of 310 documents
Self-Organization of 2-Acylaminopyridines in the Solid State and in Solution
2010
Aggregation of 2-acylaminopyridines and their 6-methyl derivatives in chloroform solution was studied by (1)H, (13)C, and (15)N NMR spectroscopies. The results were compared with (13)C and (15)N CPMAS NMR and IR spectral as well as with X-ray structural data. Intermolecular interactions in solution and in solid state were found to have a similar nature. Relatively strong N(amide)-H···N(pyridine) intermolecular hydrogen bonds enable dimerization to take place. Steric interactions in N-pivaloyl- and N-1-adamantylcarbonyl as well as that caused by the 6-methyl group hinder formation of the dimeric aggregates stabilized by the N(amide)-H···N(pyridine) intermolecular hydrogen bonds. In general, …
Palladium(II)-Stabilized Pyridine-2-Diazotates: Synthesis, Structural Characterization, and Cytotoxicity Studies
2018
Well-defined diazotates are scarce. Here we report the synthesis of unprecedented homoleptic palladium(II) diazotate complexes. The palladium(II)-mediated nitrosylation of 2-aminopyridines with NaNO2 results in the formation of metal-stabilized diazotates, which were found to be cytotoxic to human ovarian cancer cells.
Hypertrophic agonists induce the binding of c-Fos to an AP-1 site in cardiac myocytes: implications for the expression of GLUT1
2003
Objectives: Serum is among the agents known to induce hypertrophy of cardiac myocytes, which occurs concomitant with an increase in AP-1-mediated transcription. We have examined if this effect correlates with changes in the relative abundance of particular AP-1 heterodimers, as their exact composition under these conditions is unknown. Furthermore, we obtained insight on the specific role of c-Fos from studying the induction of the glucose transporter GLUT1 by serum in fibroblasts. Methods: We characterised the AP-1 heterodimers expressed in neonatal cardiac myocytes by supershift electrophoretic mobility shift assay (EMSA) analysis. Quantitative changes in transcription were measured using…
Sorafenib, but not sunitinib, affects function of dendritic cells and induction of primary immune responses
2008
AbstractThe tyrosine kinase inhibitors sorafenib and sunitinib are approved for the treatment of patients with malignant diseases. To analyze the possible use of these compounds in combination with immunotherapeutic approaches, we analyzed the effects of both inhibitors on the immunostimulatory capacity of human dendritic cells (DCs) and the induction of primary immune responses in vivo. Sorafenib, but not sunitinib, inhibits function of DCs, characterized by reduced secretion of cytokines and expression of CD1a, major histocompatibility complex, and costimulatory molecules in response to TLR ligands as well as by their impaired ability to migrate and stimulate T-cell responses. These inhib…
Novel inhibitors in development for hepatocellular carcinoma
2010
The multikinase inhibitor sorafenib was the first agent to demonstrate a survival benefit for patients with locally advanced or metastatic hepatocellular carcinoma (HCC). Although sorafenib represents a landmark in the treatment of HCC and proved molecularly targeted therapy to be effective in this disease, it represents just the first step towards an improvement in systemic therapy. Since then, novel inhibitors have been evaluated in early clinical trials, showing potential activity.This article aims to review novel inhibitors emerging in the field of advanced HCC. An Internet-based search was performed to identify abstracts, clinical trials ( www.clinicaltrials.gov , last accessed 30 Nove…
Proton tautomerism in 2-nitramino-C-nitropyridine derivatives - Experimental and quantum chemical study
2019
Abstract The structures of 2-nitramino-3-nitropyridine and 2-nitramino-5-nitropyridine have been characterized by X-ray diffraction and Density Functional Theory (DFT) studies. In the crystals, both compounds exist as the imino forms. The DFT calculations were performed in order to explore the amino-imino tautomerism of the studied compounds in the gas phase and the influence of solvent polarity on the tautomeric equilibrium. The Harmonic Oscillator Model of Aromaticity index (HOMA) and Nucleus Independent Chemical Shift (NICS) calculated for the pyridine rings of the studied systems, demonstrated a noticeable decrease in aromaticity of the imino forms. This study showed also that the highe…
A catalytic highly enantioselective direct synthesis of 2-bromo-2-nitroalkan-1-ols through a Henry reaction.
2008
Highly enantiomerically enriched 2-bromo-2-nitroalkan-1-ols are prepared by direct condensation of aliphatic and aromatic aldehydes with bromonitromethane in the presence of a catalytic amount of copper(II) acetate and a C1-symmetric camphorderived amino pyridine ligand. Blay Llinares, Gonzalo, Gonzalo.Blay@uv.es ; Hernandez Olmos, Victor, Victor.Hernandez@uv.es ; Pedro Llinares, Jose Ramon, Jose.R.Pedro@uv.es
Triazolopyridines. Part 27.1 the preparation of novel 6,7-dihydro[1,2,3] triazolo[1,5-a]pyridines
2010
A very efficient synthesis of the unknown family of 6,7-dihydro[1,2,3]triazolo[1,5-a]pyridines from [1,2,3]triazolo[1,5-a]pyridines have been developed, and a mechanism for their formation has been proposed. Their behaviour with NBS to give 4,5-dibromo substituted-4,5,6,7-tetrahydro-[1,2,3]triazolo[1,5-a]pyridines is studied. Abarca Gonzalez, Belen, Belen.Abarca@uv.es ; Adam Ortiz, Rosa, Rosa.Adam@uv.es ; Ballesteros Campos, Rafael, Rafael.Ballesteros@uv.es
Efficacy and safety of regorafenib for advanced gastrointestinal stromal tumours after failure of imatinib and sunitinib (GRID): an international, mu…
2013
Contains fulltext : 118365.pdf (Publisher’s version ) (Closed access) BACKGROUND: Until now, only imatinib and sunitinib have proven clinical benefit in patients with gastrointestinal stromal tumours (GIST), but almost all metastatic GIST eventually develop resistance to these agents, resulting in fatal disease progression. We aimed to assess efficacy and safety of regorafenib in patients with metastatic or unresectable GIST progressing after failure of at least imatinib and sunitinib. METHODS: We did this phase 3 trial at 57 hospitals in 17 countries. Patients with histologically confirmed, metastatic or unresectable GIST, with failure of at least previous imatinib and sunitinib were rando…
Final results of the European Advanced Renal Cell Carcinoma Sorafenib (EU-ARCCS) expanded-access study: a large open-label study in diverse community…
2011
Background The European Advanced Renal Cell Carcinoma Sorafenib (EU-ARCCS) expanded-access study provided sorafenib to advanced renal cell carcinoma (RCC) patients in whom previous systemic therapy had failed. The study assessed the safety and use of sorafenib for the treatment of advanced RCC in a large community-based patient population across 11 countries in Europe. Patients and methods EU-ARCCS was a single-arm, open-label trial of sorafenib in advanced RCC patients. End points included safety, time to progression, progression-free survival (PFS), and disease control rate (DCR). Subgroup analyses included age, Eastern Cooperative Oncology Group performance status, histology, prior thera…