bluuebunny/crossref_metadata_2025_split huggingface dataset:
ChemInform Abstract: “On Water” Direct Pd‐Catalyzed C—H Arylation of Thiazolo[5,4‐d]pyrimidine Derivatives.
Authors: Su Ye‐Xiang , Deng Ya‐Hui , Ma Ting‐Ting , Li Yu‐Yan , Sun Li‐Ping 
Published: October 2012

AbstractThe reaction requires 2 equiv.
ChemInform Abstract: 1,3‐Oxazinan‐2‐ones from Amines and 1,3‐Diols Through Dialkyl Carbonate Chemistry.
Authors: McElroy Con Robert , Arico Fabio , Tundo Pietro 
Published: October 2012

AbstractThe one‐pot base‐mediated cascade reaction is tested with 4 diesters and the mixed derivative (VI) bearing a sterically hindered ‐tBu group is found to be the most efficient one.
ChemInform Abstract: Oxidative Metal‐Free Cross‐Coupling of Secondary Phosphine Chalcogenides and Benzenediols: Synthesis of Phosphinochalcogenoic O‐Diesters.
Authors: Gusarova Nina K. , Volkov Pavel A. , Ivanova Nina I. , Larina Ludmila I. , Trofimov Boris A. 
Published: October 2012

AbstractHitherto unknown phosphinochalcogenoic O‐diesters (III) are obtained under mild conditions.
ChemInform Abstract: The New Cassane‐Type Diterpenes from Caesalpinia minax.
Authors: Ma Guo‐Xu , Yuan Jing‐Quan , Cao Li , Yang Jun‐Shan , Xu Xu‐Dong 
Published: October 2012

AbstractNeocaesalpin S (Ia), T (Ib), U (Ic) and V (II) show mild antiproliferative activities against liver cancer (HepG‐2) and breast cancer (MCF‐7).
ChemInform Abstract: Recognition of myo‐Inositol 1,4,5‐Trisphosphate Using a Fluorescent Imidazolium Receptor.
Authors: Jung Ji Young , Jun Eun Jin , Kwon Yong‐Uk , Yoon Juyoung 
Published: October 2012

AbstractDerivative (I) shows a selective fluorescent change with D‐myo‐IP3 among the various IP series, pyrophosphate, and ATP.
Using sampled information: is it enough for the sparse matrix–vector product locality optimization?
Authors: Pichel Juan C. , Lorenzo Juan A. , Rivera Francisco F. , Heras Dora B. , Pena Tomás F. 
Published: October 2012

SUMMARYOne of the main factors that affect the performance of the sparse matrix–vector product (SpMV) is the low data reuse caused by the irregular and indirect memory access patterns. Different strategies to deal with this problem such as data reordering techniques have been proposed. The computational cost of these techniques is typically high because they consider all the nonzeros of the sparse matrix in order to find an appropriate permutation of rows and columns that improves the SpMV performance. In this paper, we analyze the possibility of increasing the locality of the SpMV using incomplete information in the reordering process. This partial information comes as a consequence of considering only a subset of the nonzero elements of the matrix. These nonzeros are obtained from the original matrix through a sampling process. In particular, two different sampling methods have been considered: a random sampling and an event‐based sampling using hardware counters. We have detected that a small number of samples is enough to obtain quality reorderings. As a consequence, using sampling‐based reorderings leads to noticeable performance improvements with respect to the non‐reordered matrices, reaching speedup values up to 2.1 × . In addition, an important reduction in the computational time required by the reordering technique has been observed. Copyright © 2012 John Wiley & Sons, Ltd.
Design of a 1‐GSample/s 9‐b double sampling track‐and‐hold amplifier in BiCMOS technology
Authors: Lin Hung‐Yi , Lai Yen‐Tai 
Published: October 2012

SUMMARYThis paper gives a detail presentation of a fully pseudo‐differential open‐loop BiCMOS track‐and‐hold amplifier (THA) for 9‐b operation up to 1 GSample/s. The proposed THA not only uses a double sampling technique to increase the achievable sampling frequency by a factor of two, but also employs a linearization technique to reduce the gain dependence of the THA input stage upon the input level. Moreover, timing mismatch between the clock signals of the two interleaved paths is minimized by means of a timing mismatch insensitive clock generator controlled by a common master sampling clock. The post‐layout simulation results using TSMC 75 GHz fT, 0.35‐µm SiGe BiCMOS technology show that the proposed architecture achieve a signal to noise and distortion ratio of 53.92 dB, equivalent to the effective number of bits of 8.66‐b for 58.11 MHz input frequency at 1 GSample/s. The power dissipation of the whole THA is 161.1 mW. Copyright © 2012 John Wiley & Sons, Ltd.
Companion Diagnostics and the Drug–Diagnostic Codevelopment Model
Authors: Jørgensen Jan Trøst 
Published: October 2012

Abstract

Preclinical Research

The concept of using a predictive or selective diagnostic assay in relation to drug development goes back to the 1970s when the selective estrogen receptor modulator, tamoxifen (AstraZeneca) was developed for metastatic breast cancer. Clinical data showed that the estrogen receptor status correlated well with the clinical outcome when the patients were treated with tamoxifen. Although this datum was published more than 35 years ago, the adaption of the drug–diagnostic codevelopment model has been relatively slow, and it is only within the last decade that it has gained widespread acceptance. In this model, the drug and the diagnostic are interdependent, and if the development project proves successful, the companion diagnostic assay (CoDx) will end up determining the conditions for the use of the drug. This gatekeeper role obviously requires that the CoDx assays adhere to the same strict rules and regulations that are known from the development of drugs. For any CoDx assay, it must be documented that it is robust and reliable and that it possesses clinical utility. The article focus on some of the most important aspects of the CoDx development process with emphasis on the clinical validation and clinical utility but also other critical issues such as the biomarker selection process, determination of the cut‐off value, and the analytical validation are discussed.
Ensemble Classification of Cancer Types and Biomarker Identification
Authors: Hijazi Hussein , Wu Ming , Nath Aritro , Chan Christina 
Published: October 2012

Abstract

Preclinical Research

Cancer classification is an important step in biomarker identification. Developing machine learning methods that correctly predict cancer subtypes/types can help in identifying potential cancer biomarkers. In this commentary, we presented ensemble classification approach and compared its performance with single classification approaches. Additionally, the application of cancer classification in identifying biomarkers for drug design was discussed.
Berberine Modulates Epigenetics via Inhibition of Hypoxia‐Induced Histone Lysine Demethylases Expression
Authors: Vavilala Divya Teja , Vadlapatla Ramya Krishna , Ponnaluri VK Chaithanya , Prakash Swami , Mukherji Mridul 
Published: October 2012

Abstract

Preclinical Research

Pathological neovascularization during ischemic retinopathies is the major cause of blindness. The underlying cause of neovascularization is activation of the hypoxia‐inducible factor (HIF) pathway leading to expression of pro‐angiogenic factors. Recent studies have established that histone lysine demethylases (KDMs) play an important role in the HIF‐mediated expression of pro‐angiogenic factors under hypoxic conditions. Thus, inhibitors of the HIF pathway can be used for the treatment of these debilitating diseases. Here, we show that berberine, a plant alkaloid with a long history of medicinal use, is a potent inhibitor of the HIF pathway and hypoxia‐induced expression of KDMs in a number of retinal pigment epithelial and cancer cell lines. Treating these cells with berberine leads to inhibition of KDMs‐mediated induction of pro‐angiogenic genes (adrenomedullin and growth differentiation factor 15) under hypoxic conditions. Because berberine has been used in eyedrops to treat trachoma, our results suggest that its proper delivery to the back of the eye may treat retinal and choroidal neovascularization during ischemic retinopathies.
Analysis of 30 synthetic cannabinoids in oral fluid using liquid chromatography‐electrospray ionization tandem mass spectrometry
Authors: Kneisel Stefan , Auwärter Volker , Kempf Jürgen 
Published: October 2012

In recent years, the analysis of synthetic cannabinoids in human specimens has gained enormous importance in the broad field of drug testing. Nevertheless, the considerable structural diversity among synthetic cannabinoids already identified in ‘herbal mixtures’ hampers the development of comprehensive analytical methods. As the identification of the main metabolites of newly appearing substances is very laborious and time‐consuming, the detection of the parent compounds in blood samples is the current approach of choice for drug abstinence testing. Whenever blood sampling is not possible however, the need for alternative matrices arises.In this article, we present a fully validated liquid chromatography‐electrospray ionization tandem mass spectrometry (LC/ESI‐MS/MS) method for the analysis of 30 synthetic cannabinoids in oral fluid samples collected with the Dräger DCD 5000 collection device. The method proved to be suitable for the quantification of 28 substances. The limits of detection were in the range from 0.015 to 0.9 ng/ml, while the lower limits of quantification ranged from 0.15 to 3.0 ng/ml. The method was successfully applied to 264 authentic samples during routine analysis. A total of 31 samples (12%) was tested positive for at least one of the following synthetic cannabinoids: AM‐694, AM‐2201, JWH‐018, JWH‐019, JWH‐081, JWH‐122, JWH‐203, JWH‐210, JWH‐250, JWH‐307, MAM‐2201, and RCS‐4. Given that stabilization of the collection pads after sampling is warranted, the collection device provides satisfactory sensitivity. Hence, whenever blood sampling is not possible, the Dräger DCD 5000 collection device offers a good tool for the analysis of synthetic cannabinoids in oral fluid in the broad field of drug testing. Copyright © 2012 John Wiley & Sons, Ltd.
Regulation of the specialized DNA polymerase eta: Revisiting the biological relevance of its PCNA‐ and ubiquitin‐binding motifs
Authors: Despras Emmanuelle , Delrieu Noémie , Garandeau Charlène , Ahmed‐Seghir Sana , Kannouche Patricia L. 
Published: October 2012

AbstractDuring translesion synthesis (TLS), low‐fidelity polymerases of the Y‐family polymerases bypass DNA damages that block the progression of conventional processive DNA polymerases, thereby allowing the completion of DNA replication. Among the TLS polymerases, DNA polymerase eta (polη) performs nucleotide incorporation past ultraviolet (UV) photoproducts and is deficient in cancer‐prone xeroderma pigmentosum variant (XPV) syndrome. Upon UV irradiation, the DNA sliding clamp PCNA is monoubiquitylated on its conserved Lys‐164. This event is considered to facilitate the TLS process in vivo since polη preferentially interacts with monoubiquitylated PCNA through its ubiquitin‐binding domain (UBZ) as well as its PCNA interacting peptide (PIP)‐box. However, recent observations questioned this model. Therefore, in this study, we re‐examined the relative contribution of the regulatory UBZ and PIP domains of polη in response to UVC. We show that simultaneous invalidation of both motifs confers sensitivity to UVC, sensitization by low concentrations of caffeine, prolonged inhibition of DNA synthesis and persistent S phase checkpoint activation, all characteristic features of XPV cells. While each domain is essential for efficient accumulation of polη in replication factories, mutational inactivation of UBZ or PIP motif only confers a slight sensitivity to UVC indicating that, although informative, polη focus analysis is not a reliable tool to assess the polη's ability to function in TLS in vivo. Taken together, these data indicate that PIP and UBZ motifs are not required for recruitment but for retention of polη at sites of stalled replication forks. We propose that this is a way to ensure that a sufficient amount of the protein is available for its bypass function. Environ. Mol. Mutagen., 2012. © 2012 Wiley Periodicals, Inc.
Safety Behaviours in Eating Disorders: Factor Structure and Clinical Validation of the Brief Safety Behaviours Scale
Authors: Waller Glenn , Kyriacou Marcoulides Olivia 
Published: October 2012

AbstractThis study examined the utility of a transdiagnostic measure of safety behaviours [Brief Safety Behaviours Scale (BSBS)] in eating disorders. Prior to treatment, a group of 102 women with eating disorders completed the BSBS and well‐validated measures of eating pathology, anxiety and intolerance of uncertainty. The BSBS had three factors, suggesting that avoidant, checking and social safety behaviours are distinct constructs in the eating disorders. This three‐scale scoring system showed greater clinical precision in correlations with eating pathology than the original two‐scale version. The pattern of safety behaviours in the eating disorders is more specific than had previously been shown in other clinical samples. While it is important to consider eating‐related safety behaviours in the eating disorders (e.g. restriction, body checking), it is also necessary to consider the role of generic safety behaviours when assessing, formulating and treating eating disorders. Copyright © 2012 John Wiley & Sons, Ltd and Eating Disorders Association.
Long‐range transcriptional regulation of breast cancer genes
Authors: Betts Joshua A. , French Juliet D. , Brown Melissa A. , Edwards Stacey L. 
Published: October 2012

AbstractBreast cancer is a major health problem and understanding the genetic basis of this disease is crucial for predicting risk and developing effective targeted therapeutics. Several breast cancer predisposing genes have been identified, but mutations in the coding regions of these genes only accounts for a small proportion of risk. Research now suggests that combinations of multiple non‐coding changes in breast cancer susceptibility genes, which cause moderate alterations in gene expression, will be responsible for the remaining inherited risk. These non‐coding changes will include variants in proximal and distal transcriptional and post‐transcriptional regulatory elements and may affect the levels and function of trans‐acting factors, including proteins and RNAs, which act on these elements. Somatic changes in such elements and factors have also been associated with breast cancer progression. With the recent advent of techniques allowing the detection of long‐range DNA interactions spanning the human genome, it has become increasingly clear that long‐range regulatory elements constitute an important mechanism for gene regulation. Recent studies have identified several such elements that are important for regulating genes involved in breast cancer, raising the possibility that defects in these sequences may contribute to breast cancer predisposition and progression. In this review, we discuss the emerging functions of cis‐regulatory elements and a subset of trans‐acting factors in breast tumorigenesis. We also discuss some recent progress in our understanding of how dysregulation in these transcriptional components may contribute to breast cancer, and the potential implications for molecular diagnosis, prognosis prediction, and the treatment of this disease. © 2012 Wiley Periodicals, Inc.
Gold(I)‐Catalyzed Cyclodehydration Enabled by the Triisopropylsilyl Group: A Synthetically Versatile Methodology
Authors: Usanov Dmitry L. , Naodovic Marina , Brasholz Malte , Yamamoto Hisashi 
Published: October 2012

AbstractIntroduction of a triisopropylsilyl group into allyl and allenyl carbinols greatly enhances the efficiency of gold(I)‐catalyzed cyclodehydration, which can provide rapid access to a library of various compounds including 1H‐indenes (Table 2 and Scheme 5), benzofulvenes (Table 3), indan‐2‐ones (Scheme 2), fulvenes (Table 4), cyclopentadienes (Table 4), 5H‐dibenzo[a,c][7]annulenes (Scheme 6) and dibenzosuberones (Scheme 6). The developed method enables unprecedented product generality for several classes of cyclodehydration reactions, which is particularly notable for the preparation of 1H‐indenes. The first synthesis of non‐benzo‐fused fulvenes via cyclodehydration of allenyl vinyl carbinols could be accomplished. The protocol is remarkable for mild conditions, operational convenience, and easy access to starting materials.
dl‐Ribose Crystal Structures: the GlassCrystal Transformation
Authors: Zandomeneghi Giorgia , Schweizer W. Bernd , Gilmour Ryan , Meier Beat H. , Dunitz Jack D. 
Published: October 2012

AbstractWe present two crystal structures of dl‐ribose and a first glimpse into the mechanism of the glasscrystal transformation of sugars.
C1‐Symmetric Bicyclo[2.2.2]octa‐2,5‐diene (bod*) Ligands in Rhodium‐Catalyzed Asymmetric 1,4‐Addition of Arylboronic Acids to Enones and 1,2‐Addition to N‐[(4‐Nitrophenyl)sulfonyl]imines
Authors: Brönnimann Rebecca , Chun Sothys , Marti Roger , Abele Stefan 
Published: October 2012

AbstractA set of ten C1‐symmetric chiral bicyclo[2.2.2]octa‐2,5‐dienes (bod*) 2 (Fig. 1) were tested as ligands in Rh‐catalyzed arylation reactions. The 1,4‐addition of arylboronic acids to cyclohex‐2‐en‐1‐one, cyclopent‐2‐en‐1‐one, and tert‐butyl cinnamate proceeded smoothly with excellent enantioselectivities (up to 99% ee; Tables 1–3). The challenging 1,2‐addition of triphenylboroxine to N‐[(4‐nitrophenyl)sulfonyl]imines yielded the product in high yield and in good enantioselectivity (up to 92% ee; Table 4). Generally, the use of C1‐symmetric chiral bod* ligands bearing bulky substituents resulted in lower enantioselectivities, whereas several electron‐poor and electron‐rich bod* ligands gave higher enantioselectivities than the benchmark ligands reported in literature.
Cyclization of (2‐Alkenylphenyl)carbonyl Compounds to Polycyclic Arenes Catalyzed by Copper(II) Trifluoromethanesulfonate or Trifluoromethanesulfuric Acid
Authors: Liu Wei‐Min , Tnay Ya Lin , Gan Kian Ping , Liu Zhen‐Hong , Tyan Wan Huei , Narasaka Koichi 
Published: October 2012

AbstractVarious polycyclic arenes, such as naphthalenes, tetrahydroantharacenes, tetrahydrotetracenes, dihydropentacenes, and dihydropentaphenes are prepared from 2‐alkenylphenyl ketones and aldehydes by the catalytic use of copper(II) trifluoromethanesulfonate (Cu(OTf)2) or trifluoromethanesulfuric acid (TfOH).
Secondary Amine‐Catalyzed Asymmetric γ‐Alkylation of α‐Branched Enals via Dienamine Activation
Authors: Silvi Mattia , Cassani Carlo , Moran Antonio , Melchiorre Paolo 
Published: October 2012

AbstractThe direct and enantioselective γ‐alkylation of α‐substituted α,β‐unsaturated aldehydes proceeding under dienamine catalysis is described. We have found that the Seebach modification of the diphenyl‐prolinol silyl ether catalyst in combination with saccharin as an acidic additive promotes an SN1 alkylation pathway, while ensuring complete γ‐site selectivity and a high stereocontrol. Theoretical and spectroscopic investigations have provided insights into the conformational behavior of the covalent dienamine intermediate derived from the condensation of 2‐methylpent‐2‐enal and the chiral amine. Implications for the mechanism of stereoinduction are discussed.
A Total Synthesis of Aliskiren
Authors: Nam Gyeok , Ko Soo Y. 
Published: October 2012

AbstractA total synthesis of aliskiren (20) was accomplished. A key in our synthesis was to use the symmetric trans‐cisoid‐trans‐bis‐lactone 1 as a precursor. It was expediently prepared by three different routes (Scheme 2). Appending the end groups and functional group transformations completed the synthesis (Scheme 3).
Synthesis of (1α)‐1,25‐Dihydroxyvitamin D3 with a β‐Positioned Seven‐Carbon Side Chain at C(12)
Authors: Carballa Diego M. , Rumbo Antonio , Torneiro Mercedes , Maestro Miguel , Mouriño Antonio 
Published: October 2012

AbstractA convergent synthesis of an analogue of (1α)‐1,25‐dihydroxyvitamin D3 (1b) with a C7 side chain at C(12), i.e., of 5 (Fig.), is described. A key step of the synthesis is the assembly of the triene system by a PdII‐catalyzed ring closure of an enol triflate (‘bottom’ fragment) followed by coupling of the resulting PdII intermediate with an alkenylboronate (‘upper’ fragment) (Scheme 2). The synthetic strategy allows isotopic labelling at the end of the synthesis.
Kinetic Resolution of Racemic Secondary Benzylic Alcohols by the Enantioselective Esterification Using Pyridine‐3‐carboxylic Anhydride (3‐PCA) with Chiral Acyl‐Transfer Catalysts
Authors: Shiina Isamu , Nakata Kenya , Ono Keisuke , Mukaiyama Teruaki 
Published: October 2012

AbstractPyridine‐3‐carboxylic anhydride (3‐PCA) was found to function as an efficient coupling reagent for the preparation of carboxylic esters from various carboxylic acids with alcohols under mild conditions by a simple experimental procedure. This novel condensation reagent 3‐PCA was applicable not only for the synthesis of achiral carboxylic esters catalyzed by 4‐(dimethylamino)pyridine (DMAP) but also for the production of chiral carboxylic esters by the combination of chiral nucleophilic catalyst, such as tetramisole (=2,3,5,6‐tetrahydro‐6‐phenylimidazo[2,1‐b][1,3]thiazole) derivatives. An efficient kinetic resolution of racemic benzylic alcohols with achiral carboxylic acids was achieved by using 3‐PCA in the presence of (R)‐benzotetramisole ((R)‐BTM), and a variety of optically active carboxylic esters were produced with high enantiomeric excesses by this new chiral induction system without using a tertiary amine.
A Hydrogen Chloride‐Free Pinner Reaction Promoted by Lewis Acids
Authors: Pfaff Dominik , Nemecek Gregor , Podlech Joachim 
Published: October 2012

AbstractA hydrogen chloride‐free variation of the Pinner reaction was developed, in which alcohols react with carbonitriles to furnish carboxylates. Best results were achieved with aliphatic alcohols, and aliphatic or benzylic nitriles in the presence of 2 equiv. of trimethylsilyl triflate (Me3SiOTf). With these substrates, yields exceeding 80% were achieved. A strictly neutral variation of this protocol is possible, when 1 equiv. of Et3N is added to the reaction mixture.
A Manifold Three‐Step Synthetic Route to Polycyclic Annulated Hydantoins via Cyclic Imines
Authors: Brockmeyer Fabian , Kröger Denis , Stalling Timo , Ullrich Pasqual , Martens Jürgen 
Published: October 2012

AbstractA new three‐step synthetic pathway to generate polycyclic annulated hydantoins via rarely investigated heterocyclic imines is described. This procedure includes a one‐pot reaction forming imines as precursor structures (e.g., Asinger reaction), followed by an Ugi reaction to build up a bisamide structure that allows a ring‐closing reaction to the targeted hydantoins via substitution. This pathway leads to a multiplicity of substances with a potential pharmacological activity.
Standards, Policy Paradoxes, and the New Literacy Studies: A Call to Professional Political Action
Authors: Burns Leslie David 
Published: October 2012

AbstractIn this commentary, the author uses New Literacy Studies theories to examine the Common Core State Standards Initiative (CCSSI). Through analysis and critique of the CCSSI and related reform efforts underway in the United States, the author discusses how policy mandates can and have resulted in paradoxes. Corporate discourses of effectiveness and bureaucracy (intentionally or otherwise) undercut the use of research‐based knowledge for literacy education reform. Consequently, professional literacy educators are positioned to subordinate themselves in the governance of their own profession despite statements by reform leaders that they must have the autonomy to make expert decisions that help students learn and practice literacy in contemporary society. The author calls for organizations like the International Reading Association to act politically and strategically, create knowledge, mobilize members, and educate stakeholders so that policy reforms become more equitable, just, and successful for the ends they are intended to meet.