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91.
Oxidative Metabolism of Ferrocene Analogues of Tamoxifen: Characterization and Antiproliferative Activities of the Metabolites 下载免费PDF全文
Dr. Marie‐Aude Richard Dr. Didier Hamels Dr. Pascal Pigeon Dr. Siden Top Dr. Patrick M. Dansette Hui Zhi Shirley Lee Dr. Anne Vessières Dr. Daniel Mansuy Prof. Gérard Jaouen 《ChemMedChem》2015,10(6):981-990
Ferrociphenols have been found to have high antiproliferative activity against estrogen‐independent breast cancer cells. The rat and human liver microsome‐mediated metabolism of three compounds of the ferrocifen ( FC ) family, 1,1‐bis(4‐hydroxyphenyl)‐2‐ferrocenyl‐but‐1‐ene ( FC1 ), 1‐(4‐hydroxyphenyl)‐1‐(phenyl)‐2‐ferrocenyl‐but‐1‐ene ( FC2 ), and 1‐[4‐(3‐dimethylaminopropoxy)phenyl]‐1‐(4‐hydroxyphenyl)‐2‐ferrocenyl‐but‐1‐ene ( FC3 ), was studied. Three main metabolite classes were identified: quinone methides ( QM s) deriving from two‐electron oxidation of FC s, cyclic indene products ( CP s) deriving from acid‐catalyzed cyclization of QM s, and allylic alcohols ( AA s) deriving from hydroxylation of FC s. These metabolites are generated by cytochromes P450 (P450s), as shown by experiments with either N‐benzylimidazole as a P450 inhibitor or recombinant human P450s. Such P450‐dependent oxidation of the phenol function and hydroxylation of the allylic CH2 group of FC s leads to the formation of QM and AA metabolites, respectively. Some of the new ferrociphenols obtained in this study were found to exhibit remarkable antiproliferative effects toward MDA‐MB‐231 hormone‐independent breast cancer cells. 相似文献
92.
Influence of the Multivalency of Ultrashort Arg‐Trp‐Based Antimicrobial Peptides (AMP) on Their Antibacterial Activity 下载免费PDF全文
Barbara C. Hoffknecht Dennis J. Worm Sandra Bobersky Pascal Prochnow Prof. Dr. Julia E. Bandow Prof. Dr. Nils Metzler‐Nolte 《ChemMedChem》2015,10(9):1564-1569
Peptide dendrimers are a class of molecules of high interest in the search for new antibiotics. We used microwave‐assisted, copper(I)‐catalyzed alkyne–azide cycloaddition (CuAAC; “click” chemistry) for the simple and versatile synthesis of a new class of multivalent antimicrobial peptides (AMPs) containing solely arginine and tryptophan residues. To investigate the influence of multivalency on antibacterial activity, short solid‐phase‐ synthesized azide‐modified Arg‐Trp‐containing peptides were “clicked” to three different alkyne‐modified benzene scaffolds to access scaffolds with one, two, or three peptides. The antibacterial activity of 15 new AMPs was investigated by minimal inhibitory concentration (MIC) assays on five different bacterial strains, including a multidrug‐resistant Staphylococcus aureus (MRSA) strain. With ultrashort (2–3 residues) peptides, a clear synergistic effect of the trivalent display was observed, whereas this effect was not apparent with longer peptides. The best candidates showed activities in the low‐micromolar range against Gram‐positive MRSA. Surprisingly, the best activity against Gram‐negative Acinetobacter baumannii was observed with an ultrashort dipeptide on the trivalent scaffold (MIC: 7.5 μM ). The hemolytic activity was explored for the three most active peptides. At concentrations ten times the MIC values, <1 % hemolysis of red blood cells was observed. 相似文献
93.
An antibacterial peptide (AMP), i.e., nisin, was covalently bound to gelatin through a protein–protein coupling. Various reaction conditions were tested to study and optimize parameters of grafting e.g., orientation and density of AMP, which could impact the final antibacterial activity of the modified biopolymer. Modification was investigated by Fourier transform infrared (FT‐IR) spectroscopy and zeta potential. The antibacterial activity of the nisin‐enriched gelatin was evaluated against two staphylococci bacterial strains, i.e., Staphylococus epidermidis and Staphylococcus aureus. A higher activity was found for gelatin modified at pH = 7.4 revealing an influence of the nisin orientation on the protein antibacterial property. © 2014 Wiley Periodicals, Inc. J. Appl. Polym. Sci. 2015 , 132, 41825. 相似文献
94.
According to the revised 1996 IPCC guidelines, several emission factors are needed to calculate national inventories of N2O emissions from agriculture. To estimate the direct N2O emissions from mineral soils, an emission factor of 0.0125 kg N2O-N per kg N applied is currently being used. From recent literature data it was clearly shown that real N2O emissions could differ substantially from this value. Based on the IPCC methodology an inventory of N2O emission from agriculture in Europe (EU-15) has been made. In 1996, the N2O emission was estimated at 672 Gg N2O-N. The N2O emission per country varied between 10 and 177 Gg N2O-N. The N2O emission per ha agricultural land in the various countries varied between 1.7 and 14.2 kg N2O-N ha−1. Highest N2O emissions per ha were found in countries with a high agricultural intensity, such as the Netherlands, Belgium-Luxembourg,
Denmark and Germany. Agricultural soils are a sink for atmospheric methane. An oxidation capacity of 2.5 and 1.5 kg CH4 ha−1 yr−1 was put forward for grasslands and arable land, respectively. Based on land use data of 1993, the CH4 sink of agricultural lands in EU-15 was estimated at 303.5 Gg CH4. In general, it could be concluded that N2O emissions from soils (327 Tg CO2 equivalents) are far more important than its sink function for CH4 (6.3 Tg CO2 equivalents).
This revised version was published online in August 2006 with corrections to the Cover Date. 相似文献
95.
Polymerization shrinkage of methacrylate‐based dental composites remains a major concern in restorative dentistry. Cyclic monomers that undergo ring‐opening polymerization are known to exhibit reduced polymerization shrinkage compared to methacrylates. In this article, the synthesis of four crosslinking 1,1‐disubstituted 2‐vinylcyclopropanes bearing rigid spacers is described. These monomers were synthesized by esterification of 1‐ethoxycarbonyl‐2‐vinylcyclopropane‐1‐carboxylic acid with the corresponding diols. The photopolymerization kinetics of these monomers was investigated by photo‐differential scanning calorimeter using bis(4‐methoxybenzoyl)diethylgermane as the photoinitiator. The synthesized vinylcyclopropanes (VCPs) were shown to be more reactive than the frequently used reactive diluent triethylene glycol dimethacrylate. Composites based on these VCPs showed good mechanical properties and exhibited a significantly reduced volumetric shrinkage and shrinkage stress compared to a corresponding dimethacrylate‐based restorative material. This work highlights the excellent potential of VCPs as alternatives to methacrylates in the development of low‐shrinkage dental composites. © 2017 Wiley Periodicals, Inc. J. Appl. Polym. Sci. 2017 , 134, 45577. 相似文献
96.
José Antonio Díaz Elżbieta Skrzyńska Soraya Zaid Jean‐Sébastien Girardon Mickaël Capron Franck Dumeignil Pascal Fongarland 《Journal of chemical technology and biotechnology (Oxford, Oxfordshire : 1986)》2017,92(9):i-i
The cover image, by José Antonio Díaz et al., is based on the Research Article Kinetic modelling of the glycerol oxidation in the liquid phase: comparison of Pt, Au and Ag AS active phases, DOI: 10.1002/jctb.5296 . Photo Credit: CNRS Photothèque / Cyril FRESILLON.
97.
98.
Absorption methods for the determination of mass transfer parameters of packing internals: A literature review 下载免费PDF全文
Laszlo Hegely John Roesler Pascal Alix David Rouzineau Michel Meyer 《American Institute of Chemical Engineers》2017,63(8):3246-3275
Methods for the determination of mass‐transfer coefficients and effective interfacial areas in packed absorption columns are reviewed. For each parameter, the methods are grouped into categories on the basis of their physical principle; the chemical systems used, experimental protocol, and the advantages and inconveniences are discussed. The treatment of end effects, the influence of packed bed height, and the recent efforts in standardization of measurement methods are also treated. The aim of the review is to give a broad overview of the methods used in literature in the last eight decades, some of which might be reconsidered in the light of modern measurement techniques and to evaluate them in relation to precision, practicality and hazardousness thereby to facilitate the search for reliable, precise, and convenient experimental practices. © 2017 American Institute of Chemical Engineers AIChE J, 63: 3246–3275, 2017 相似文献
99.
Dr. Mohamed Ettaoussi Dr. Ahmed Sabaouni Dr. Basile Pérès Elodie Landagaray Dr. Olivier Nosjean Dr. Jean A. Boutin Dr. Daniel‐Henri Caignard Dr. Philippe Delagrange Prof. Pascal Berthelot Dr. Saïd Yous 《ChemMedChem》2013,8(11):1830-1845
Agomelatine is a naphthalenic analogue of melatonin that is in clinical use for the treatment of major depressive disorders. Interestingly, while agomelatine exhibits potent affinity for melatonin receptors, it binds with only moderate affinity to the serotonin 5‐HT2C receptor. Optimization of agomelatine toward this target could further potentiate its clinical efficacy. To explore this hypothesis and to access derivatives in which a key point of agomelatine metabolism is blocked, a series of naphthalenic derivatives was designed and synthesized as novel analogues of agomelatine. Most of the prepared compounds exhibited good binding affinity at the melatonin MT1 and MT2 receptor subtypes. Two compounds, an acetamide and an acrylamide derivative, exhibited good binding affinities at both the human melatonin (MT) receptors and the serotonin 5‐HT2C receptor subtype, with pKi values of 7.96 and 7.95 against MT1, 7.86 and 8.68 against MT2, and 6.64 and 6.44 against 5‐HT2C, respectively. 相似文献
100.
Andreas Haase Pascal Hesse Lars Brommer Olaf Jacobs Clarissa Abetz Ulrich A. Handge Adriana Boschetti‐de‐Fierro Volker Abetz 《大分子材料与工程》2013,298(3):292-302
This study presents a nanocomposite manufacturing route starting from non‐functionalized nanosilica and SAN surface modification via “grafting from” ATRP up to processing of transparent polycarbonate and glycol modified poly(ethylene terephthalate) nanocomposites. Synthesis limitations of low molecular weight graft SAN derived from “classical” ATRP are overcome by employment of the emerging ARGET ATRP. Mechanical investigations of polycarbonate and glycol modified poly(ethylene terephthalate) nanocomposites present up to 80% enhancement of creep performance and additionally 70% enhancement against wear abrasion for glycol modified poly(ethylene terephthalate) nanocomposites. Strength and tensile modulus are only moderately influenced by the addition of nanoparticles. Morphological studies confirm that the present modification route is able to create uniform dispersions of single particles and small particle aggregates in polymer matrices.