bluuebunny/crossref_metadata_2025_split huggingface dataset:
Synthesis and evaluation of boron folates for Boron-Neutron-Capture-Therapy (BNCT)
Authors: Kettenbach Kathrin , Schieferstein Hanno , Grunewald Catrin , Iffland Dorothée , Reffert Laura M. , Hampel Gabriele , Schütz Christian L. , Bings Nicolas H. , Ross Tobias L. 
Published: September 2015

Abstract
Boron neutron capture therapy (BNCT) employs 10B-pharmaceuticals administered for the treatment of malignancies, and
subsequently irradiated with thermal neutrons. So far, clinical established pharmaceuticals like boron phenylalanine (BPA) or sodium
boron mercaptate (BSH) use imperfect (BPA) or passive (BSH) targeting for accumulation at target sites. Due to the need of a selective
transportation of boron drugs into cancer cells and sparing healthy tissues, we combined the BNCT approach with the specific and
effective folate receptor (FR) targeting concept. The FR is overexpressed on many human carcinomas and provides a selective and
specific target for molecular imaging as well as for tumor therapy. We synthesized and characterized a carborane-folate as well as
a BSH-folate to study their in vitro characteristics and their potential as new boron-carriers for BNCT. Uptake studies were carried
out using human KB cells showing a significant increase of the boron content in cells and demonstrating the successful combination of
active FR-targeting and BNCT.
Interfacial Dilational Rheology of the Novel Zwitterionic Surfactants
Authors: Hu Songshuang , Li Zhenquan , Song Xinwang , Dong Linfang , Liu Yan , Zhang Lei , Zhang Lu , Zhao Sui 
Published: September 2015

Abstract
The dilational rheological properties of series branched betaine
surfactants: Guerbet p-(n-tetradecyl)-benzyl carboxybetaine
(C14GCB), Guerbet p-(n-dodecyl)-benzyl polyoxyethylene
ether(2) carboxybetaine (C12GE2CB), Guerbet
p-(n-tetradecyl)-benzyl polyoxyethylene ether(2) carboxybetaine
(C14GCB) and Guerbet p-(n-hexadecyl)-benzyl polyoxyethylene
ether(2) carboxybetaine (C16GCB), were investigated by
drop shape analysis method at the water-decane interface. The
dilational properties of surfactants were investigated as a function
of time, frequency and concentration. The experimental results show
that the time dependence was complex. It was also found that the
dilational modulus were almost independent of frequency in the
experimental concentration range for C14GE2CB and
C16GE2CB, while the dilational modulus of
C14GCB and C12GE2CB increased with the
increase of frequency, sharing the same results with conventional
zwitterionic surfactants. The results indicated the appearance of
a more elastic film for the C14GE2CB and
C16GE2CB due to the internal compression and expansion
of oxyethylene units (EO). On the other hand, the surfactant with
branched alkyl chain came forth a higher maximum value of dilational
modulus compared with the straight chain surfactants with the
increase of concentration, which means the branching of alkyl chain
was another important factor to control the interfacial film.
Les formes différenciées d’usages de produits psychoactifs au travail : les cas des bars-restaurants et des chantiers du bâtiment
Authors: Ngo Nguene Marie Rosaire 
Published: September 2015

Cet article rend compte des formes différenciées d’usages d’alcool, de cocaïne et de cannabis des salariés des bars-restaurants et chantiers du bâtiment en s’appuyant sur des matériaux d’enquêtes essentiellement qualitatifs, recueillis dans le cadre d’un travail de thèse en cours 1 . Les consommations de produits psychoactifs dans ces organisations suivent des logiques collectives et individuelles qu’il convient d’expliquer. Pour cela, nos analyses prendront conjointement en compte les conditions de travail proprement dites (travail de nuit dans le secteur bar-restauration, pénibilité physique dans les chantiers du bâtiment, par exemple) ; les dynamiques sociales et culturelles des usages de substances psychoactives, leurs propriétés physiques et chimiques ; les caractéristiques sociales des salariés, examinés à travers leurs trajectoires personnelles et professionnelles, en prenant en compte les effets d’âge et de génération.
Mythe et histoire dans l’exegèse médiévalede la genèse
Authors: Dahan Gilbert 
Published: September 2015

Les exégètes médiévaux ont-ils une attitude particulière à l’égard des récits de la Bible que nous faisons aujourd’hui entrer dans la catégorie du « mythe » ? On voudrait répondre à cette question à partir de l’étude des généalogies des chapitres 4 et 5 de la Genèse dans les commentaires composés entre le xii e et le xiv e siècles en Occident. Celles du chapitre 4 (v. 17-22) sont considérées comme un mythe sur les origines de la culture – la vie pastorale, le travail des métaux, la musique, le tissage –, celles du chapitre 5 posent des problèmes divers, notamment du fait de la longueur de la vie des personnages nommés. Il semble que les commentateurs du Moyen Âge soient moins sensibles à la dimension « historique » de ces textes qu’aux enseignements que nous pouvons en tirer sur les fondements de la conduite humaine. L’analyse qu’ils font des structures de ces textes (utilisant notamment la valeur symbolique attachée aux nombres et mettant en relief les différences d’agencement) et les applications tropologiques qu’ils en tirent, puisznt dans l’Écriture sainte les enseignements d’une Parole adressée en permanence à l’homme, permettent de constater que les procédures qu’ils mettent en œuvre sont proches de celles d’une certaine analyse des mythes aujourd’hui.
Liver histopathological changes in Clarias gariepinus exposed to ethanol extract of Adenium obesum stem bark
Authors: Abalaka S. , Fatihu M. , Ibrahim N. , Ambali S. 
Published: September 2015

Abstract
Introduction: Histopathological effects of ethanol extract of Adenium obesum stem bark on the liver of Clariasgariepinus was investigated over a 96-h exposure period as an effective organic piscicide. Materials and Methods: An acute static toxicity bioassay was performed after a preliminary concentration range finding test was conducted. Results: Exposed fish showed adaptation behavioural changes with those of respiratory distress and abnormal nervous signs of toxicity, which was concentration-dependent. Mortality was recorded in some of the exposed fish while a median lethal concentration of 7.15 mgL-1 was established for the extract in the exposed fish. Non-significant (p>0.05) changes were recorded in serum aspartate aminotransferase, alanine aminotransferase and alkaline phosphatase activities of the exposed ish. Moderate liver damage was observed in the exposed fish based on the degree of tissue change (DTC) grading where significant (p<0.05) differences were observed between the DTC of the exposed groups and the control. Conclusion: Ethanol extract of A. obesum stem bark was toxic to the exposed fish with evidence of hepatotoxicity and therefore, can be used to eradicate the hardy C.gariepinus from aquatic environments.
Observations of the summer breakup of an Arctic sea ice cover
Authors: Arntsen Alexandra E. , Song Arnold J. , Perovich Donald K. , Richter‐Menge Jacqueline A. 
Published: September 2015

AbstractThe Arctic sea ice cover evolves dramatically through the summer melt season. Floe size distribution (FSD) is a critical parameter used to examine this change as the ice cover transitions from large rectilinear plates in spring to an ensemble of discrete rounded floes by midsummer. The FSD at a given time impacts the dynamic and thermodynamic behavior of the ice cover. Focusing on the seasonal marginal ice zone in the Beaufort and Chukchi Seas from May to September 2014, we present qualitative and quantitative results derived from National Technical Means high‐resolution imagery and supported by ice mass balance buoy data. Results indicate that as melt accelerates, floe breaking pattern, and therefore FSD, is heavily influenced by the distribution of melt ponds. Discrete element model results using morphological conditions derived from analyzed satellite imagery confirmed that breaking occurs along ponds and perpendicular to applied stress.
Unraveling the missing link of ENSO control over the Indian monsoon rainfall
Authors: Dwivedi Suneet , Goswami B. N. , Kucharski Fred 
Published: September 2015

AbstractUsing long daily rainfall (113 years) data, clear evidence of modulation of the statistics of subseasonal active and break spells of the Indian summer monsoon rainfall (ISMR) by the El Niño–Southern Oscillation (ENSO) is unraveled. We show that during the El Niño (La Nina) years, the frequency of longer break (active) spells and shorter active (break) spells increases substantially, while the frequency of shorter breaks (active) and longer active (break) spells decreases compared to ENSO neutral years. It is shown that the large‐scale teleconnection through which ENSO weakens (strengthens) the ISMR through shortening (lengthening) of the length of rainy season (LRS) also creates a background for modulation of the statistics of subseasonal spells leading to a further reduction (increase) in the ISMR during El Niño (La Niña) years. Our findings indicate that the “statistics of subseasonal spells” is predictable, brightening the prospect of seasonal prediction of the ISMR.
Quantifying contributions of model processes to the surface temperature bias in FGOALS‐g2
Authors: Liu Bo , Zhou Tianjun , Lu Jianhua 
Published: September 2015

AbstractTo quantify the annual mean surface temperature bias due to various processes in Flexible Global Ocean‐Atmosphere‐Land‐System model, Grid point version 2 (FGOALS‐g2), the climate feedback‐response analysis method (CFRAM) is used to isolate contributions from both radiative and nonradiative processes in the model by comparing the model simulation with ERA‐Interim reanalysis. The observed surface temperature bias is decomposed into seven partial temperature biases associated with surface albedo, water vapor, cloud, both surface sensible and latent heat fluxes, land/ocean heat transport processes, and atmospheric transport processes. The global mean cold bias (−1.39 K) is mostly attributed to surface albedo and land/ocean heat transport processes while surface latent heat fluxes tend to weaken this bias. Cloud‐induced bias is dominated by shortwave cloud radiative effect (SWCRE) over low‐latitudes and longwave cloud radiative effect (LWCRE) over high latitudes. The mixed layer depth (MLD) bias is consistent with the bias due to ocean heat transport over North Pacific, North Atlantic, and the Southern Ocean. On global scale, contributions of radiative processes and nonradiative processes to the total observed cold bias are comparable, but tend to compensate each other over most regions except for the northern high latitudes. We suggest that the improvements in tropical clouds in the model may significantly decrease the global temperature bias through the interaction between clouds and circulation.
Global sensitivity of parabolic equation radar wave propagation simulation to sea state and atmospheric refractivity structure
Authors: Lentini N. E. , Hackett E. E. 
Published: September 2015

AbstractInadequate representation of the environment is a limitation for prediction of radar system performance as well as for validation of propagation codes. To improve understanding of how different environmental effects/parameters compete and compare, this study examines the sensitivity of radar wave propagation to a suite of environmental parameters for low grazing angle near‐surface radar systems at 3–15 GHz at horizontal and vertical polarizations. A global sensitivity analysis method is used, which accounts for parameter interactions, and propagation is modeled using the parabolic equation method. Environmental parameters examined include eight sea state parameters and eight parameters characterizing the vertical structure and character of range‐independent refractivity profiles. The relative importance of parameters varies more with frequency than polarization, and parameter interactions are found to be significant. Atmospheric mixed layer parameters are found to be the most sensitive, particularly the thickness of the mixed layer. The most significant ocean surface parameter is swell period, although sea directionality is important at 3 GHz and sea surface roughness and salinity are important at 9 and 15 GHz. Because of the spatial variability of sensitivity throughout the domain, regional analysis is performed to determine the most important parameters in different regions of the domain (1000 m in altitude and 60 km in range). These regional sensitivity results, along with those for the whole domain, provide guidance on prioritization of environmental characterization in numerical weather prediction and inversion studies (e.g., refractivity from clutter studies), which are two common methods currently used to address environmental effects on propagation.
3‐Naphthylindole Construction by Rhodium(II)‐Catalyzed Regioselective Direct Arylation of Indoles with 1‐Diazonaphthalen‐2‐(1H)‐ones
Authors: Baral Ek Raj , Lee Yong Rok , Kim Sung Hong 
Published: September 2015

AbstractThe regioselective direct 3‐arylation of indoles with 1‐diazonaphthalen‐2‐(1H)‐ones was developed by means of a rhodium(II) pivalate‐catalyzed cross‐coupling reaction. This procedure provided a variety of novel 3‐naphthylindoles in high yield. The direct coupling of benzofuran, pyrrole or furan with 1‐diazonaphthalen‐2‐(1H)‐ones afforded 2‐ or 3‐naphthyl substituted heterocycles.magnified image
On‐Column Reaction Set‐Up for High‐Throughput Screenings and Mechanistic Investigations
Authors: Stockinger Skrollan , Troendlin Johannes , Rominger Frank , Trapp Oliver 
Published: September 2015

AbstractA screening platform, which offers a high‐throughput approach as well as an easy investigation of kinetic isotope effects, applicable to a wide range of reactions is presented. To illustrate the high potential of this approach, the asymmetric transfer hydrogenation of methyl benzoylformate with copper(II) bis(oxazoline) and Hantzsch ester was examined. Accordingly, the enantioselectivities of the reaction performed on‐column in a microcapillary were comparable to standard reaction conditions, however, we were able achieve catalysis and analysis in a single step in less than 30 min. The throughput can be increased by simultaneous investigation of different substrates without increasing the overall analysis time. Use of di‐deuterated Hantzsch ester allowed us to investigate the kinetic isotope effect of the transfer hydrogenation reaction only requiring a minute amount of the deuterated transfer hydrogenation reagent. Hence we were able to get further insights into the mechanism of the asymmetric transfer hydrogenation using Hantzsch ester as hydrogen source. The here presented technique is broadly applicable to study isotope effects on a very small scale, which is a rapid and an inexpensive alternative compared to conventional experiments.magnified image
Enantioselective Palladium‐Catalyzed Heck–Heck Cascade Reactions: Ready Access to the Tetracyclic Core of Lycorane Alkaloids
Authors: Coya Estibaliz , Sotomayor Nuria , Lete Esther 
Published: September 2015

AbstractA rapid and efficient access to a wide variety of enantiomerically enriched C‐11b substituted lycorane analogues can be achieved via a catalytic asymmetric Heck–Heck 6‐exo/6‐endo cascade reaction in the presence of (R)‐BINAP.magnified image
Brønsted Acid‐Promoted Cascade Alkylation/Cyclization of Pyrroles with N,N‐Dimethylaminomethyleneglutaconic Acid Dinitrile: A Concise Route to Cyclopenta[b]pyrroles
Authors: Wu Kaikai , Wu Ping , Chen Jiping , Sun Chenglin , Yu Zhengkun 
Published: September 2015

AbstractA Brønsted acid (p‐TsOH⋅H2O) promoted alkylation/cyclization cascade reaction of pyrroles with N,N‐dimethylaminomethyleneglutaconic acid dinitrile was efficiently realized to afford functionalized cyclopenta[b]pyrroles with excellent diastereoselectivity. Deamination of the corresponding ammonium salts of the cyclopenta[b]pyrroles with methyl iodide led to dihydrocyclopenta[c]pyrroles. The cascade reaction pathway was confirmed by isolation and transformation of the reaction intermediate, i.e., the 2‐alkylated pyrrole.magnified image
Rhodium(III)‐Catalyzed Redox‐Neutral CH Annulation of Arylnitrones and Alkynes for the Synthesis of Indole Derivatives
Authors: Zhou Zhi , Liu Guixia , Chen Yan , Lu Xiyan 
Published: September 2015

AbstractBy using a nitrone as the oxidizing directing group, a mild, practical and efficient rhodium(III)‐catalyzed CH functionalization for the synthesis of indole derivatives has been developed. This reaction obviates the need for an external oxidant and shows good functional group tolerance. The employment of a sterically hindered Mes group on the carbon center of the nitrone is crucial to produce indoles in high yield.magnified image
Synthesis, Characterization, and Optical Performance of a Novel Fluorescent Waterborne Polyurethane
Authors: Tian Saiqi , Zhang Peikun , Fan Haojun , Chen Yi , Yan Jun , Shi Bi 
Published: September 2015

ABSTRACTA fluorescent fluorescent waterborne polyurethane (FWPU) was synthesized by conjugating fluorescer, isodium 4,4′‐bis[4‐anilino‐6‐hydroxyethylamino‐6‐(2‐choloronilino‐1,3,5‐triazin‐2‐yl)amino]stilbene‐2,2′‐disulphonate (RSW), into polyurethane backbone as a chain extender. The expected structure of FWPU was confirmed by Fourier transform infrared, 1H nuclear magnetic resonance, and UV−vis spectrophotometer, and the effect of fluorescer content, temperature, as well as quencher on the fluorescence performances of FWPU was investigated in detail. Results reveal that covalently conjugation has unconspicuous effect on optical performance, and FWPU shows similar fluorescence intensity to fluorescer RSW except for a red shift of about 10 nm in maximum absorption wavelengths. Further study finds that there is a positive correlation between the concentration of fluorescer and the fluorescence intensity of FWPU; however, the opposite effect is obtained when the concentration exceeds 1 × 10−5 mol/L, which is attributed to the concentration self‐quenching. Although high temperature will decrease the intensity of fluorescence, the fluorescence components in FWPU shows high resistance to fluorescence quencher and thermal decomposition as a consequence of chemical combination with the polymer chain.
Trends of occupational fatalities involving machines, United States, 1992–2010
Authors: Marsh Suzanne M. , Fosbroke David E. 
Published: September 2015

BackgroundThis paper describes trends of occupational machine‐related fatalities from 1992–2010. We examine temporal patterns by worker demographics, machine types (e.g., stationary, mobile), and industries.MethodsWe analyzed fatalities from Census of Fatal Occupational Injuries data provided by the Bureau of Labor Statistics to the National Institute for Occupational Safety and Health. We used injury source to identify machine‐related incidents and Poisson regression to assess trends over the 19‐year period.ResultsThere was an average annual decrease of 2.8% in overall machine‐related fatality rates from 1992 through 2010. Mobile machine‐related fatality rates decreased an average of 2.6% annually and stationary machine‐related rates decreased an average of 3.5% annually. Groups that continued to be at high risk included older workers; self‐employed; and workers in agriculture/forestry/fishing, construction, and mining.ConclusionAddressing dangers posed by tractors, excavators, and other mobile machines needs to continue. High‐risk worker groups should receive targeted information on machine safety. Am. J. Ind. Med. 58:1160–1173, 2015. Published 2015. This article is a U.S. Government work and is in the public domain in the USA.
N‐Heterocyclic‐Carbene‐Catalyzed Stereoselective Annulations: An Efficient Strategy for the Synthesis of Chromeno[4,3‐b]pyrrolidine Derivatives
Authors: Qi Jing , Duan Xiao‐Yong , Cao Li‐Li , Wang Wen‐Ying 
Published: September 2015

AbstractAn N‐heterocyclic‐carbene‐catalyzed annulation of alkynyl aldehydes and o‐hydroxy aromatic aldimines for the construction of chromeno[4,3‐b]pyrrolidine derivatives has been developed. This cascade Michael/Mannich/lactonization process constructs three new bonds and three consecutive stereogenic centers in a single step with excellent diastereoselectivity and low catalyst loading.
Rhodium(III)‐Catalyzed Allylic C(sp3)–H Activation of Alkenyl Sulfonamides: Unexpected Formation of Azabicycles
Authors: Archambeau Alexis , Rovis Tomislav 
Published: September 2015

AbstractUnsaturated N‐sulfonamides undergo a RhIII‐ catalyzed allylic C(sp3)H activation followed by insertion with an exogenous internal alkyne. The reaction generates [3.3.0], [4.3.0], and [5.3.0] azabicyclic structures with excellent diastereoselectivity. Deuterium labeling experiments implicate a 1,3‐Rh shift as a key step in the mechanism.
Rerouting Electron Transfer in Molecular Assemblies by Redox‐Pair Matching
Authors: Balgley Renata , Shankar Sreejith , Lahav Michal , van der Boom Milko E. 
Published: September 2015

AbstractWe demonstrate how the distance over which electron transfer occurs through organic materials can be controlled and extended. Coating of conductive surfaces with nanoscale layers of redox‐active metal complexes allows the electrochemical addressing of distant layers that are otherwise electrochemically silent. Our materials can pass electrons selectively in directions that are determined by positioning of layers of metal complexes and the distances between them. These electron‐transfer processes can be made dominantly uni‐ or bidirectional. The design involves 1) a set of isostructural metal complexes with different electron affinities, 2) a scalable metal–organic spacer, and 3) a versatile assembly approach that allows systematic variation of composition, structure, and electron‐transfer properties. We control the electrochemical communication between interfaces by the deposition sequence and the spacer length, therefore we are able to program the bulk properties of the assemblies.
Activity‐Directed Synthesis with Intermolecular Reactions: Development of a Fragment into a Range of Androgen Receptor Agonists
Authors: Karageorgis George , Dow Mark , Aimon Anthony , Warriner Stuart , Nelson Adam 
Published: September 2015

AbstractActivity‐directed synthesis (ADS), a novel discovery approach in which bioactive molecules emerge in parallel with associated syntheses, was exploited to develop a weakly binding fragment into novel androgen receptor agonists. Harnessing promiscuous intermolecular reactions of carbenoid compounds enabled highly efficient exploration of chemical space. Four substrates were prepared, yet exploited in 326 reactions to explore diverse chemical space; guided by bioactivity alone, the products of just nine of the reactions were purified to reveal diverse novel agonists with up to 125‐fold improved activity. Remarkably, one agonist stemmed from a novel enantioselective transformation; this is the first time that an asymmetric reaction has been discovered solely on the basis of the biological activity of the product. It was shown that ADS is a significant addition to the lead generation toolkit, enabling the efficient and rapid discovery of novel, yet synthetically accessible, bioactive chemotypes.
Palladium‐Catalyzed Heteroarylation and Concomitant ortho‐Alkylation of Aryl Iodides
Authors: Lei Chuanhu , Jin Xiaojia , Zhou Jianrong (Steve) 
Published: September 2015

AbstractThree‐component couplings were achieved from common aryl halides, alkyl halides, and heteroarenes under palladium and norbornene co‐catalysis. The reaction forges hindered aryl–heteroaryl bonds and introduces ortho‐alkyl groups to aryl rings. Various heterocycles such as oxazoles, thiazoles and thiophenes underwent efficient coupling. The heteroarenes were deprotonated in situ by bases without the assistance of palladium catalysts.