bluuebunny/crossref_metadata_2025_split huggingface dataset:
Analysis of Wild-Type and Mutant SL3-3 Murine Leukemia Virus Insertions in the c-mycPromoter during Lymphomagenesis Reveals Target Site Hot Spots, Virus-Dependent Patterns, and Frequent Error-Prone Gap Repair
Authors: Nielsen Anne Ahlmann , Sørensen Annette Balle , Schmidt Jörg , Pedersen Finn Skou 
Published: December 2004

ABSTRACTThe murine leukemia retrovirus SL3-3 induces lymphomas in the T-cell compartment of the hematopoetic system when it is injected into newborn mice of susceptible strains. Previously, our laboratory reported on a deletion mutant of SL3-3 that induces T-cell tumors faster than the wild-type virus (S. Ethelberg, A. B. Sørensen, J. Schmidt, A. Luz, and F. S. Pedersen, J. Virol. 71:9796-9799, 1997). PCR analyses of proviral integrations in the promoter region of the c-mycproto-oncogene in lymphomas induced by wild-type SL3-3 [SL3-3(wt)] and the enhancer deletion mutant displayed a difference in targeting frequency into this locus. We here report on patterns of proviral insertions into the c-mycpromoter region from SL3-3(wt), the faster variant, as well as other enhancer variants from a total of approximately 250 tumors. The analysis reveals (i) several integration site hot spots in the c-mycpromoter region, (ii) differences in integration patterns between SL3-3(wt) and enhancer deletion mutant viruses, (iii) a correlation between tumor latency and the number of proviral insertions into the c-mycpromoter, and (iv) a [5′-(A/C/G)TA(C/G/T)-3′] integration site consensus sequence. Unexpectedly, about 12% of the sequenced insertions were associated with point mutations in the direct repeat flanking the provirus. Based on these results, we propose a model for error-prone gap repair of host-provirus junctions.
Vitreous humour as a complementary sample to blood for the detection/confirmation of diazepam: ante-mortem and post-mortem studies in an animal model
Authors: Teixeira H M , Reis F , Proença P , Ramos P , Quińtela O , López-Rivadulla M , Marques E , Vieira D N 
Published: December 2004

The quantification of medical or toxic substances in vitreous humour (VH) could be very useful in forensic toxicology when blood sample determinations are impossible due to absence or deterioration. However, few studies have been made in this area and even fewer have tried to find a relationship between drug levels in both samples. To determine a correlation ratio between blood and VH diazepam (DZ) levels, we performed an experimental study using rabbits administered with a sub-toxic dose of DZ under known and controlled conditions. Blood and VH samples were collected 0.5, 1, 2, 3 and 6 hours after the drug administration in order to determine DZ and its main active metabolite, desmethyldiazepam (DMD). In addition, we have studied an animal group sacrificed 2 hours after intramuscular (i.m.) drug administration with blood and VH collection 24 hours later, to evaluate the existence of possible post-mortem changes. After DZ administration, a fast absorption phase was observed with a plasma Cmax value 1 hour after, followed by a rapid concentration decrease, with a half-life of 1 hour, indicating that, besides elimination, a fast distribution to other organs and tissues and/or hepatic metabolism occurred. Diazepam Cmax value in VH was achieved between 1 and 2 hours, when plasma concentrations had already decreased to half the value. The plasma/VH DZ ratio calculated at this time was 10. In the post-mortem study, while plasma DZ concentration at 24 hours was smaller, DMD levels were higher than those at the time of death. In the VH, both DZ and DMD concentrations at 24 hours were higher than those obtained at the time of death. That is, in both fluids DZ and DMD concentrations were different from those at the time of death and post-mortem distribution and redistribution phenomena occurred. The combination of antemortem and post-mortem studies has allowed the determination of a correlation ratio for DZ in the rabbit of 6×, comparing the concentrations in VH collected 24 hours after death with the concentrations detected in plasma at the time of death. This study opens new perspectives for the use of VH as a complementary sample to blood for DZ detection and confirmation. The putative relevance of the correlation ratio obtained, for forensic toxicology practice with medical substances, namely benzodiazepines, recommends further studies in humans.
Physical and chemical stability of palonosetron HCl with cisplatin, carboplatin, and oxaliplatin during simulated Y-site administration
Authors: Trissel Lawrence A. , Zhang Yanping 
Published: December 2004

The objective of this study was to evaluate the physical and chemical stability of undiluted palonosetron HCl 50 mcg/mL with cisplatin 0.5 mg/mL, carboplatin 5 mg/mL, and with oxaliplatin 0.5 mg/mL in infusion solutions during simulated Y-site administration. Triplicate test samples were prepared by admixing 7.5 mL of palonosetron HCl with 7.5 mL of the cisplatin, carboplatin, and oxaliplatin dilutions. Physical stability was assessed using a multistep evaluation procedure that included both turbidimetric and particulate measurement as well as visual inspection. Chemical stability was assessed using stability-indicating HPLC analytical techniques based on the determination of drug concentrations. Evaluations were performed initially upon mixing and 1 and 4 hours after mixing. The samples were clear and colourless when viewed in normal fluorescent room light and when viewed with a Tyndall beam. Measured turbidity remained unchanged and particulate content was low and exhibited little change. HPLC analysis found palonosetron HCl, cisplatin, carboplatin, and oxaliplatin remained stable throughout the 4-hour test with no drug loss. Palonosetron HCl is physically compatible and chemically stable with cisplatin, carboplatin, and oxaliplatin during Y-site administration.
Cobalt‐Mediated Mizoroki–Heck‐Type Reaction of Epoxide with Styrene
Authors: Ikeda Yousuke , Yorimitsu Hideki , Shinokubo Hiroshi , Oshima Koichiro 
Published: December 2004

AbstractTreatment of a mixture of epoxide and styrene with trimethylsilylmethylmagnesium bromide in the presence of a cobalt‐phosphine complex afforded homocinnamyl alcohol in good yield. The reaction should begin with ring opening of the epoxide by the action of magnesium bromide which leads to the formation of a magnesium 2‐bromoethoxide derivative and not with a direct single electron transfer from a cobalt complex to the epoxide.
Palladium‐Indium‐Indium(III) Chloride‐Mediated Allyl Cross‐Coupling Reactions Using Allyl Acetates
Authors: Lee Phil Ho , Seomoon Dong , Lee Kooyeon , Kim Sundae , Kim Hyunseok , Kim Hyun , Shim Eunkyong , Lee Miae , Lee Seokju , Kim Misook , Sridhar Madabhushi 
Published: December 2004

AbstractAllylindiums in situ generated by reductive transmetalation of π‐allylpalladium(II) complexes, obtained from allyl acetates and palladium(0) catalyst, with indium and indium(III) chloride are effective nucleophilic cross‐coupling partners in Pd‐catalyzed allyl cross‐coupling reactions with a variety of electrophilic cross‐coupling partners.
Sonogashira Cross‐Coupling Reactions Catalysed by Copper‐Free Palladium Zeolites
Authors: Djakovitch Laurent , Rollet Patrick 
Published: December 2004

AbstractA heterogeneous copper‐free [Pd(NH3)4]2+/(NH4)Y catalyst was employed to achieve the heterogeneous Sonogashira reaction of aryl halides with terminal alkynes. Several reaction parameters like solvent, base and temperature were evaluated. When optimised, the coupling reaction of bromobenzene with phenylacetylene gave a 45% yield of diphenylacetylene within 3 h using only 1 mol % Pd. This catalyst was successfully applied to the coupling reaction of a range of aryl iodides and bromides: aryl iodides and activated aryl bromides gave almost quantitative yields and non‐activated aryl bromides led to reasonable yields (20% to 45%). This heterogeneous [Pd(NH3)4]2+/(NH4)Y catalyst was shown to be efficient, stable towards leaching and recyclable for the copper‐free Sonogashira reaction.
Rhodium‐Catalyzed Coupling Reaction of Aroyl Chlorides with Alkenes
Authors: Sugihara Toru , Satoh Tetsuya , Miura Masahiro , Nomura Masakatsu 
Published: December 2004

AbstractAroyl chlorides react with acyclic and cyclic alkenes in the presence of a rhodium catalyst to give Mizoroki–Heck type and cyclization products, respectively. A rhodium‐ethylene complex, [{RhCl(C2H4)2}2], showed excellent performance for these reactions. Notably, the reactions can be conducted effectively under base‐ and phosphane‐free conditions.
Palladium‐Catalyzed Intramolecular Coupling of Amino‐Tethered Vinyl Halides with Ketones, Esters, and Nitriles Using Potassium Phenoxide as the Base
Authors: Solé Daniel , Urbaneja Xavier , Bonjoch Josep 
Published: December 2004

AbstractVinyl halides undergo intramolecular coupling with amino‐tethered ketones, esters, and nitriles in the presence of a palladium catalyst and potassium phenoxide as the base. This reaction constitutes a useful methodology for the synthesis of monocyclic, bridged, and spirocyclic nitrogen‐containing compounds.
Industrial R&D on Catalytic CC and CN Coupling Reactions: A Personal Account on Goals, Approaches and Results
Authors: Blaser Hans‐Ulrich , Indolese Adriano , Naud Frédéric , Nettekoven Ulrike , Schnyder Anita 
Published: December 2004

AbstractR&D issues for the application of Pd‐ and Ni‐catalyzed CC and CN coupling reactions in the fine chemicals industry are discussed. In a first part, some background is given on industrial R&D and the role of CC and CN coupling for preparative applications is described. The following principal approaches to industrial research are illustrated with relevant examples from the literature and from our own laboratories: i) development of catalysts and catalytic methodologies with industrial potential; ii) finding shorter routes to target molecules using catalytic methods; iii) development of industrial catalytic processes in multi‐step syntheses.
Combinatorial Explosion in Homogeneous Catalysis: Screening 60,000 Cross‐Coupling Reactions
Authors: Burello Enrico , Farrusseng David , Rothenberg Gadi 
Published: December 2004

AbstractA new approach to the selection of Heck cross‐coupling catalysts and reaction conditions is presented, based on a quantitative structure‐activity relationship (QSAR) descriptor set that is coupled to linear and non‐linear analysis models. A set of steric and electronic descriptors is defined and calculated. The correlations between ligands, substrates, catalyst precursors and reaction conditions in a dataset of 412 Heck reactions are then analyzed using artificial neural networks, classification tree methods, and linear models. The regression and classification models are powerful, with prediction confidence levels as high as 93%. These models are then used to predict the performance (turnover numbers and turnover frequencies) of 60,000 combinations of virtual catalysts and reaction conditions in silico. Furthermore, the models are used to pinpoint mechanistic effects, in this case the important role that small palladium clusters play in Heck cross‐coupling. The pros and cons of linear and non‐linear models and the application of this approach to the selection of new experiments in high‐throughput systems are discussed.
Chelation‐Induced Catalytic Multiple Arylation of Allylic 2‐Pyridyl Sulfones
Authors: Llamas Tomás , Arrayás Ramón Gómez , Carretero Juan Carlos 
Published: December 2004

AbstractThe development of a chelation‐assisted, transition metal‐catalyzed protocol for the sequential multiarylation of cyclic allyl sulfones is described. The metal‐coordinating ability of the 2‐pyridyl group on the sulfone promotes the otherwise difficult intermolecular Heck monoarylation and diarylation of trisubstituted alkenes, as well as the copper‐catalyzed allylic arylation with Grignard reagents.
Terminal Heck Vinylations of Chelating Vinyl Ethers
Authors: Stadler Alexander , von Schenck Henrik , Vallin Karl S. A. , Larhed Mats , Hallberg Anders 
Published: December 2004

AbstractTerminal chelation‐controlled Heck vinylations of electron‐rich amino‐functionalized vinyl ethers were performed with high regioselectivity furnishing moderate to good isolated yields of the corresponding 1‐alkoxy‐1,3‐butadienes. DFT calculations support an amine‐palladium(II) coordination strength reactivity/selectivity rationale, where the dimethylamino group was the preferred metal presenting functionality. Controlled microwave heating effectively accelerated these palladium‐catalyzed reactions and full conversion could be achieved within 30 minutes. Subsequent Diels–Alder reactions with dimethyl acetylenedicarboxylate under microwave irradiation resulted exclusively in partly aromatized bi‐ and tricyclic compounds by elimination of the aminoalkoxy group. Thus, the selected dimethylamino auxiliary both controlled the regiochemistry in the palladium‐catalyzed vinylation and was easily displaced in the aromatization process.
Palladium‐Catalyzed Cross‐Coupling Reaction by Means of Organogermanium Trichlorides
Authors: Enokido Tatsuki , Fugami Keigo , Endo Mayuko , Kameyama Masayuki , Kosugi Masanori 
Published: December 2004

AbstractEasily accessible arylgermanium trichlorides were found to undergo palladium‐catalyzed cross‐coupling reactions with aryl bromides and iodides in good yields. The reaction is performed in an aqueous medium with sodium hydroxide as an activator. Some base‐sensitive functionalities such as acetyl and trifluoromethyl survived the reaction.
Palladium‐Catalyzed Heck and Carbonylation Reactions of a Dinaphthaleneiodonium Salt Forming Functionalized 2‐Iodo‐1,1′‐binaphthyls
Authors: Kina Asato , Miki Hiroyuki , Cho Yong‐Hwan , Hayashi Tamio 
Published: December 2004

AbstractThe Heck‐type olefination and carbonylation of a binaphthaleneiodonium salt 1 in the presence of a palladium catalyst gave high yields of the corresponding 2‐iodo‐2′‐functionalized‐1,1′‐binaphthyls with high selectivity.
Palladium‐Catalyzed Cross‐Coupling Reactions of Substituted Aryl(dimethyl)silanols
Authors: Denmark Scott E. , Ober Michael H. 
Published: December 2004

AbstractCesium carbonate and cesium hydroxide monohydrate are effective activators for the palladium‐catalyzed cross‐coupling of aryl(dimethyl)silanols with substituted aryl halides. Extensive optimization studies led to the identification of key variables (solvent, catalyst, additive, and hydration level) that influence the rate and selectivity of the process. Manipulation of these factors provides an effective coupling method of wide scope and generality. Electron‐rich aryl(dimethyl)silanols undergo cross‐coupling with aryl iodides and aryl bromides in high yields and high selectivity for the desired cross‐coupling products. Alternatively, high yields of cross‐coupling products could be obtained with electron‐poor or ortho‐substituted aryl(dimethyl)silanols when activated with cesium hydroxide monohydrate.
Dialkylphosphinoimidazoles as New Ligands for Palladium‐Catalyzed Coupling Reactions of Aryl Chlorides
Authors: Harkal Surendra , Rataboul Franck , Zapf Alexander , Fuhrmann Christa , Riermeier Thomas , Monsees Axel , Beller Matthias 
Published: December 2004

AbstractN‐Aryl‐2‐(dialkylphosphino)imidazoles and ‐benzimidazoles are conveniently prepared in one step from the corresponding heterocycles by selective deprotonation and quenching with chlorophosphines. The novel ligands are easily tunable and show good to excellent performance in palladium‐catalyzed Suzuki reactions and Buchwald–Hartwig aminations of aryl and heteroaryl chlorides.
Palladium‐Catalyzed CN and CO Coupling–A Practical Guide from an Industrial Vantage Point†
Authors: Schlummer Björn , Scholz Ulrich 
Published: December 2004

AbstractThe palladium‐catalyzed coupling of amines with aryl halides or aryl alcohol derivatives, commonly dubbed Buchwald–Hartwig amination, has matured from a synthetic laboratory procedure to a technique that is widely used in natural product synthesis as well as in other fields of academic interest. Furthermore, due to the versatility and reliability of this reaction, researchers in industrial environments have included this methodology in their toolbox as a standard procedure for the synthesis of amine derivatives. Therefore, it is not surprising that first industrial processes up to ton‐scale have been performed using this cross‐coupling reaction. The authors who are involved in the application of this reaction to industrial processes on this scale give an overview of the recent developments in this field of chemistry, also including fundamental principles, with a special focus on the industrial approach and issues to be considered relevant in scaling‐up this transition metal‐catalyzed chemistry. This review differs from the already existing excellent academic reviews by focusing on the practical problems arising during implementing the methodology in an industrial environment as well as giving practical hints to this end.
Catalytic Carbometalation/Cross‐Coupling Sequence across Alkynyl(2‐pyridyl)silanes Leading to a Diversity‐Oriented Synthesis of Tamoxifen‐Type Tetrasubstituted Olefins
Authors: Kamei Toshiyuki , Itami Kenichiro , Yoshida Jun‐ichi 
Published: December 2004

AbstractA general synthetic scheme for tamoxifen‐type tetrasubstituted olefins based on the novel Cu‐catalyzed carbomagnesation across alkynyl(2‐pyridyl)silane has been developed. A wide array of electronically and structurally diverse tetrasubstituted olefins can be prepared in a regiocontrolled, stereocontrolled, and diversity‐oriented manner. Noteworthy features are that (i) the three aryl groups, which are believed to be important (essential) for anti‐estrogenic activity, can be varied at will because they all stem from readily available aryl iodides, and (ii) any stereo‐ and regioisomers can, in principle, be prepared by simply changing the order use of the aryl iodides in the sequence.
Rapid lightoff of syngas production from methane: A transient product analysis
Authors: Williams Kenneth A. , Leclerc Corey A. , Schmidt Lanny D. 
Published: December 2004

AbstractSteady‐state production of syngas (CO and H2) can be attained within 10 s from room‐temperature mixtures of methane and air fed to a short‐contact‐time reactor by initially operating at combustion stoichiometry (CH4/O2 = 0.5) and then quickly switching to syngas stoichiometry (CH4/O2 = 2.0). The methane/air mixture is first ignited, forming a premixed flame upstream of the catalyst that heats the Rh‐impregnated α‐alumina foam monolith to catalytic lightoff (T > 500°C) in a few seconds. The methane/oxygen ratio is then increased to partial oxidation stoichiometry, which extinguishes the flame and effects immediate autothermal syngas production. Transient species profiles are measured with a rapid‐response mass spectrometer (response time constant ≅ 0.5 s), and catalyst temperature is measured with a thermocouple at the catalyst back face. Because the monolith thermal response time (∼ 1 s) is several orders of magnitude larger than the reaction timescales (∼ 10−12 to 10−3 s), chemistry and flow should be mathematically decoupled from local transient variations in catalyst temperature. Using this assumption, a transient temperature profile is combined with detailed surface chemistry for methane on Rh in a numerical plug‐flow model. This approach accurately reproduces the transient species profiles measured during experimental lightoff for short combustion time experiments and lends insight into how the monolith temperature develops with time. The combined experimental and numerical efforts supply useful information on the transient reactor behavior for various combustion times and identify a combustion time to avoid undershoot or overshoot in catalyst temperature and minimize start‐up time. © 2004 American Institute of Chemical Engineers AIChE J, 51: 247–260, 2005
Effect of millimeter waves on natural killer cell activation
Authors: Makar V.R. , Logani M.K. , Bhanushali A. , Kataoka M. , Ziskin M.C. 
Published: December 2004

AbstractMillimeter wave therapy (MMWT) is being widely used for the treatment of many diseases in Russia and other East European countries. MMWT has been reported to reduce the toxic effects of chemotherapy on the immune system. The present study was undertaken to investigate whether millimeter waves (MMWs) can modulate the effect of cyclophosphamide (CPA), an anticancer drug, on natural killer (NK) cell activity. NK cells play an important role in the antitumor response. MMWs were produced with a Russian‐made YAV‐1 generator. The device produced modulated 42.2 ± 0.2 GHz radiation through a 10 × 20 mm rectangular output horn. Mice, restrained in plastic tubes, were irradiated on the nasal area. Peak SAR at the skin surface and peak incident power density were measured as 622 ± 100 W/kg and 31 ± 5 mW/cm2, respectively. The maximum temperature elevation, measured at the end of 30 min, was 1 °C. The animals, restrained in plastic tubes, were irradiated on the nasal area. CPA injection (100 mg/kg) was given intraperitoneally on the second day of 3‐days exposure to MMWs. All the irradiation procedures were performed in a blinded manner. NK cell activation and cytotoxicity were measured after 2, 5, and 7 days following CPA injection. Flow cytometry of NK cells showed that CPA treatment caused a marked enhancement in NK cell activation. The level of CD69 expression, which represents a functional triggering molecule on activated NK cells, was increased in the CPA group at all the time points tested as compared to untreated mice. However, the most enhancement in CD69 expression was observed on day 7. A significant increase in TNF‐α level was also observed on day 7 following CPA administration. On the other hand, CPA caused a suppression of the cytolytic activity of NK cells. MMW irradiation of the CPA treated groups resulted in further enhancement of CD69 expression on NK cells, as well as in production of TNF‐α. Furthermore, MMW irradiation restored CPA induced suppression of the cytolytic activity of NK cells. Our results show that MMW irradiation at 42.2 GHz can up‐regulate NK cell functions. Bioelectromagnetics 26:10–19, 2005. © 2004 Wiley‐Liss, Inc.
Four‐point electrode measurement of impedance in the vicinity of bovine aorta for quasi‐static frequencies
Authors: Stiles David K. , Oakley Barbara A. 
Published: December 2004

AbstractResults are presented here of experimental measurements using a four‐point electrode technique to measure the complex impedance of bovine aorta submerged in Ringer's solution. Impedance measurements were taken at 250 μm intervals, ranging from 0 (the electrode directly on the surface of the tissue) to 10 mm. Frequencies ranged from 1 kHz to 10 MHz. Throughout this range, the measured impedance changed by an average of 400% when the electrode was 10 mm from the tissue as compared to when the electrode was in direct contact with the tissue. The change in impedance made it possible to determine when the electrode made contact with the arterial wall. Bioelectromagnetics 26:54–58, 2005. © 2004 Wiley‐Liss, Inc.