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https://www.readbyqxmd.com/read/29775970/anti-inflammatory-flavanones-and-flavanols-from-the-roots-of-pongamia-pinnata
#1
Ran Wen, Haining Lv, Yong Jiang, Pengfei Tu
A phytochemical study of the roots of Pongamia pinnata afforded 29 flavanones and flavanols, including 7 previously undescribed compounds. The structures of the isolated compounds were determined by 1D and 2D NMR and mass spectroscopy data. The absolute configurations of the compounds were assigned via analysis of the specific rotations and electronic circular dichroism spectra, application of Mosher's method, and by comparing the calculated and experimental electronic circular dichroism spectra. The isolates were evaluated for their inhibitory effects on nitric oxide production in lipopolysaccharide-stimulated BV-2 microglial cells...
May 18, 2018: Planta Medica
https://www.readbyqxmd.com/read/29775499/synthesis-spectroscopic-characterization-and-redox-reactivity-of-a-cyclic-alkyl-amino-carbene-derived-arsamethine-cyanine-dye
#2
Kortney M Melancon, M Brenton Gildner, Todd W Hudnall
In our efforts to prepare a diarsenic allotrope supported by two cyclic alkyl amino carbene (CAAC) ligands we stumbled upon the serendipitous synthesis of the first carbene-supported chloroarsinidene 3 which has been fully characterized by a combination of NMR spectroscopic and XRD methods. Although further reduction of 3 was not possible, we found that addition of a second equivalent of CAAC in refluxing toluene afforded the first example of a crystallographically characterized arsamethine cyanine dye (4)...
May 18, 2018: Chemistry: a European Journal
https://www.readbyqxmd.com/read/29775321/direct-ortho-c-h-aminoalkylation-of-2-substituted-pyridine-derivatives-catalyzed-by-yttrium-complexes-with-n-n-diarylethylenediamido-ligands
#3
Abhinanda Kundu, Mariko Inoue, Haruki Nagae, Hayato Tsurugi, Kazushi Mashima
A mixed ligated amidoyttrium complex, Y(NBn2 )(L1)(THF)2 (8, L1 = N,N'-bis(2,6-diisopropylphenyl)ethylenediamine), served as a catalyst for addition of the ortho-pyridyl C(sp2 )-H bond of 2-substituted pyridines to non-activated imines; complex 8 showed superior catalytic performance compared with Y[N(SiMe3 )2 ]3 (1) and Y[N(SiMe3 )2 ]2 (NBn2 )(THF) (2). Concerning the reaction mechanism, we conducted a stoichiometric reaction of an alkylyttrium complex, Y(CH2 SiMe3 )(L1)(THF)2 (7), with 2-ethylpyridine (4e), giving a mixture of (η3 -pyridylmethyl)yttrium complex 9 and (η2 -pyridyl)yttrium complex 10 along with elimination of SiMe4 ...
May 18, 2018: Journal of the American Chemical Society
https://www.readbyqxmd.com/read/29775310/fragment-based-discovery-of-a-potent-orally-bioavailable-inhibitor-which-modulates-the-phosphorylation-and-catalytic-activity-of-erk1-2
#4
Tom D Heightman, Valerio Berdini, Hannah Braithwaite, Ildiko Maria Buck, Megan Cassidy, Juan Castro, Aurelie Courtin, James E H Day, Charlotte East, Lynsey Fazal, Brent Graham, Charlotte M Griffiths-Jones, John F Lyons, Vanessa Martins, Sandra Muench, Joanne M Munck, David Norton, Marc O'Reilly, Nick Palmer, Puja Pathuri, Michael Reader, David C Rees, Sharna J Rich, Caroline Richardson, Harpreet Saini, Neil T Thompson, Nicola G Wallis, Hugh Walton, Nicola E Wilsher, Alison J-A Woolford, Michael Cooke, David Cousin, Stuart Onions, Jonathan Shannon, John Watts, Christopher W Murray
Aberrant activation of the MAPK pathway drives cell proliferation in multiple cancers. Inhibitors of BRAF and MEK kinases are approved for the treatment of BRAF mutant melanoma, but resistance frequently emerges, often mediated by increased signalling through ERK1/2. Here we describe the fragment based generation of ERK1/2 inhibitors which block catalytic phosphorylation of downstream substrates such as RSK but also modulate phosphorylation of ERK1/2 by MEK without directly inhibiting MEK. X-ray crystallographic and biophysical fragment screening followed by structure-guided optimization and growth from the hinge into a pocket proximal to the C-α helix afforded highly potent ERK1/2 inhibitors with excellent kinome selectivity...
May 18, 2018: Journal of Medicinal Chemistry
https://www.readbyqxmd.com/read/29775305/one-pot-synthesis-of-four-chlorin-derivatives-by-a-divergent-ylide
#5
Junior Gonzales, Naga Venkata Satya Dinesh Kumar Bhupathiraju, Daniel Hart, Man Yuen, Maria Pia Sifuentes, Bleron Samarxhiu, Mark Maranan, Naxhije Berisha, James Batteas, Charles Michael Drain
Chlorins have unique photophysical properties that are exploited in diverse biological and materials applications. De novo chlorin synthesis with specific exocyclic motifs can be challenging and many are not stable to photobleaching and/or oxidation. A facile approach to a stable synthetic chlorin with a fused N-methyl pyrrolidine uses cyclo addition of a sarcosine-based azomethine ylide on 5,10,15,20-tetrakis-(2,3,4,5,6-pentafluorophenyl)-porphyrin (TPPF20) is reported, but this approach has limitations. We report the synthesis of stable chlorin scaffolds starting with TPPF20 using a new glycine-based N-(hydroxymethyl)-N-methelenemethanideaminium ylide...
May 18, 2018: Journal of Organic Chemistry
https://www.readbyqxmd.com/read/29775301/enantioselective-synthesis-of-anti-1-2-diamines-by-cu-catalyzed-reductive-couplings-of-azadienes-with-aldimines-and-ketimines
#6
Xinxin Shao, Kangnan Li, Steven J Malcolmson
Here we report highly efficient and chemoselective azadiene-imine reductive couplings catalyzed by (Ph-BPE)Cu-H that afford anti-1,2-diamines. In all cases, reactions take place with either aldimine or ketimine electrophiles to deliver a single diastereomer of product in >95:5 er. The products' diamines are easily differentiable, facilitating down-stream synthesis.
May 18, 2018: Journal of the American Chemical Society
https://www.readbyqxmd.com/read/29775067/rhodium-iii-catalyzed-redox-neutral-synthesis-of-isoquinolinium-salts-via-c-h-activation-of-imines
#7
Miaomiao Tian, Guangfan Zheng, Xuesen Fan, Xingwei Li
Redox-neutral synthesis of isoquinolinium salts via C-H activation of pre-synthesized or in situ formed imines and coupling with α-diazo ketoesters have been realized, where a zinc salt promotes cyclization as well as provides a counter anion. Under three-component conditions, both ketone and aldehydes are viable arene sources. The coupling of imines with diazo malonates under similar conditions afforded isoquinolin-3-ones as the coupling product.
May 18, 2018: Journal of Organic Chemistry
https://www.readbyqxmd.com/read/29775046/solvent-assisted-surface-engineering-for-high-performance-all-inorganic-perovskite-nanocrystals-light-emitting-diodes
#8
Lin Wang, Baiquan Liu, Xin Zhao, Hilmi Volkan Demir, Haoshuang Gu, Handong Sun
All-inorganic cesium halide perovskite nanocrystals have attracted booming interests in optoelectronic applications for the sake of the readily adjustable bandgaps, high photoluminescence quantum yield, pure color emission and affordable cost. However, due to the ineluctable utilization of organic surfactants during the synthesis, the structural and optical properties of CsPbBr3 nanocrystals degrade upon transforming from colloidal solutions to solid thin films, which plagues the device operation. Here, we develop a novel solvent-assisted surface engineering strategy, producing high quality CsPbBr3 thin films for device applications...
May 18, 2018: ACS Applied Materials & Interfaces
https://www.readbyqxmd.com/read/29774983/mechanistic-insights-into-the-ni-catalyzed-reductive-carboxylation-of-c-o-bonds-in-aromatic-esters-with-co-2-understanding-remarkable-ligand-and-traceless-directing-group-effects
#9
Yan-Li Han, Bing-Yuan Zhao, Kun-Yao Jiang, Hui-Min Yan, Zhu-Xia Zhang, Wen-Jing Yang, Zhen Guo, Yan-Rong Li
The mechanism of the Ni0 -catalyzed reductive carboxylation reaction of C(sp2 )-O and C(sp3 )-O bonds in aromatic esters with CO2 to access valuable carboxylic acids was comprehensively studied by using DFT calculations. Computational results revealed that this transformation was composed of several key steps: C-O bond cleavage, reductive elimination, and/or CO2 insertion. Of these steps, C-O bond cleavage was found to be rate-determining, and it occurred through either oxidative addition to form a NiII intermediate, or a radical pathway that involved a bimetallic species to generate two NiI species through homolytic dissociation of the C-O bond...
May 18, 2018: Chemistry, An Asian Journal
https://www.readbyqxmd.com/read/29774922/chelation-assisted-c-n-cross-coupling-of-phosphinamides-and-aryl-boronic-acids-with-copper-powder-at-room-temperature
#10
Yao Peng, Jian Lei, Renhua Qiu, Lingteng Peng, Chak-Tong Au, Shuang-Feng Yin
A protocol for the chelation-assisted C-N cross-coupling of phosphinamides and aryl boronic acids with copper powder under an oxygen atmosphere is reported. This reaction proceeds efficiently to afford fully substituted unsymmetrical N-arylation phosphinamides at room temperature in excellent yields. Diverse unstable functional groups on the benzene ring of aryl boronic acids such as vinyl, formyl, acetyl, sulfonyl, acetylamino, cyano, nitro, and trifluoromethyl can be accommodated.
May 18, 2018: Organic & Biomolecular Chemistry
https://www.readbyqxmd.com/read/29774906/reactivity-of-a-dearomatised-pincer-co-ii-br-complex-with-pnc-nhc-donors-alkylation-and-si-h-bond-activation-via-metal-ligand-cooperation
#11
Thomas Simler, Sylvie Choua, Andreas A Danopoulos, Pierre Braunstein
The double aminolysis reaction of [Co{N(SiMe3)2}2] by the salt 1-(6-((dicyclohexylphosphaneyl)methyl)pyridin-2-yl)-3-(2,6-diisopropylphenyl)-1H-imidazol-3-ium bromide, which contains one phosphane, one pyridine and one imidazolium groups, of formula [o-Cy2PCH2(C5H3N)(o-C3H3N2DiPP)]Br and abbreviated as (CyPNpyrCim)Br, was previously shown to afford the Co(ii) complex [Co(CyP*NaCNHC)Br] (1) containing a dearomatised picolyl moiety in the tridentate, anionic donor ligand CyP*NaCNHC (Na = anionic amido, P* = vinylic P donor)...
May 18, 2018: Dalton Transactions: An International Journal of Inorganic Chemistry
https://www.readbyqxmd.com/read/29774534/adverse-selection-into-and-within-the-individual-health-insurance-market-in-california-in-2014
#12
Vicki Fung, Cassandra G K Peitzman, Julie Shi, Catherine Y Liang, William H Dow, Alan M Zaslavsky, Bruce H Fireman, Stephen F Derose, Michael E Chernew, Joseph P Newhouse, John Hsu
OBJECTIVE: The Affordable Care Act (ACA) introduced reforms to mitigate adverse selection into and within the individual insurance market. We examined the traits and predicted medical spending of enrollees in California post-ACA. DATA SOURCES: Survey of 2,103 enrollees in individual market plans, on- and off-exchange, in 2014. STUDY DESIGN: We compared actual versus potential participants using data from the 2014 California Health Interview Survey on respondents who were individually insured or uninsured...
May 17, 2018: Health Services Research
https://www.readbyqxmd.com/read/29774340/a-molecular-approach-to-magnetic-metallic-nanostructures-from-metallopolymer-precursors
#13
Qingchen Dong, Zhengong Meng, Cheuk-Lam Ho, Hongen Guo, Weiyou Yang, Ian Manners, Linli Xu, Wai-Yeung Wong
In recent years, metallopolymers have attracted much attention as precursors to generate magnetic metal/metal alloy nanoparticles (NPs) through pyrolysis or photolysis because they offer the advantages of ease of solution processability, atomic level mixing and stoichiometric control over composition. The as-generated NPs usually possess narrow size distributions with precise control of composition and density per unit area. Moreover, patterned NPs can be achieved on various substrates in this way owing to the good film-forming property of metallopolymers and such work is important for many applications based on metal nanostructures...
May 18, 2018: Chemical Society Reviews
https://www.readbyqxmd.com/read/29774176/pushing-the-limits-machine-preservation-of-the-liver-as-a-tool-to-recondition-high-risk-grafts
#14
REVIEW
Yuri L Boteon, Simon C Afford, Hynek Mergental
Purpose of the Review: Machine perfusion (MP) is a novel technology recently introduced in liver transplantation, redefining the current practice of organ preservation and pushing the limits of high-risk liver utilisation. This review highlights the key benefits of machine perfusion over conventional static cold storage (SCS), demonstrated in human liver research and clinical transplants. Recent Findings: The first clinical trials have demonstrated both safety and feasibility of MP...
2018: Current Transplantation Reports
https://www.readbyqxmd.com/read/29773978/effects-of-sevoflurane-exposure-during-mid-pregnancy-on-learning-and-memory-in-offspring-rats-beneficial-effects-of-maternal-exercise
#15
Ziyi Wu, Xingyue Li, Yi Zhang, Dongyi Tong, Lili Wang, Ping Zhao
Fetal exposure to general anesthetics may pose significant neurocognitive risks but methods to mitigate against these detrimental effects are still to be determined. We set out, therefore, to assess whether single or repeated in utero exposure to sevoflurane triggers long-term cognitive impairments in rat offspring. Since maternal exercise during pregnancy has been shown to improve cognition in offspring, we hypothesized that maternal treadmill exercise during pregnancy would protect against sevoflurane-induced neurotoxicity...
2018: Frontiers in Cellular Neuroscience
https://www.readbyqxmd.com/read/29773971/synthesis-and-polymerization-of-1-2-diallylaminoethyl-pyrimidines
#16
Jomana Elaridi, Alaa Ezzeddine, Lara Abramian, Ali Koubeissi, Nikolay Vladimirov, Kamal H Bouhadir
We report the preparation and characterization of three pyrimidine-based monomers, specifically: 1-(2-diallylaminoethyl)uracil, 1-(2-diallylaminoethyl)thymine and 1-(2-diallylaminoethyl)cytosine. Monomer synthesis was initiated by reaction of the pyrimidine with ethylene carbonate to form the hydroxyethyl adduct which was subsequently chlorinated to afford the chloroethyl intermediate. Reaction of the chloroethyl derivatives with diallylamine resulted in the desired monomers. We demonstrated a two-fold increase in the overall yield of the three monomers in comparison to reported procedures...
2018: Designed Monomers and Polymers
https://www.readbyqxmd.com/read/29773959/conservation-systematics-of-the-shield-backed-trapdoor-spiders-of-the-nigrum-group-mygalomorphae-idiopidae-idiosoma-integrative-taxonomy-reveals-a-diverse-and-threatened-fauna-from-south-western-australia
#17
Michael G Rix, Joel A Huey, Steven J B Cooper, Andrew D Austin, Mark S Harvey
The aganippine shield-backed trapdoor spiders of the monophyletic nigrum -group of Idiosoma Ausserer s. l. are revised, and 15 new species are described from Western Australia and the Eyre Peninsula of South Australia: I. arenaceum Rix & Harvey, sp. n. , I. corrugatum Rix & Harvey, sp. n. , I. clypeatum Rix & Harvey, sp. n. , I. dandaragan Rix & Harvey, sp. n. , I. formosum Rix & Harvey, sp. n. , I. gardneri Rix & Harvey, sp. n. , I. gutharuka Rix & Harvey, sp. n. , I. incomptum Rix & Harvey, sp...
2018: ZooKeys
https://www.readbyqxmd.com/read/29773592/investigating-chemoresistance-to-improve-sensitivity-of-childhood-t-cell-acute-lymphoblastic-leukemia-to-parthenolide
#18
Benjamin C Ede, Rafal R Asmaro, John P Moppett, Paraskevi Diamanti, Allison Blair
Current therapies for childhood T cell acute lymphoblastic leukemia have increased survival rates to above 85% in developed countries. Unfortunately, some patients fail to respond to therapy and many suffer from serious side effects, highlighting the need to investigate other agents to treat this disease. Parthenolide, a nuclear factor kappa B inhibitor and reactive oxygen species inducer, has been shown to have excellent anti-cancer activity in pediatric leukemia xenografts, with minimal effects on normal hemopoietic cells...
May 17, 2018: Haematologica
https://www.readbyqxmd.com/read/29773511/immobilization-does-not-disrupt-near-hand-attentional-biases
#19
Robert McManus, Laura E Thomas
Observers show biases in attention when viewing objects within versus outside of their hands' grasping space. While the hands' proximity to stimuli plays a key role in these effects, recent evidence suggests an observer's affordances for grasping actions also shape visual processing near the hands. The current study examined the relative contributions of proximity and affordances in introducing attentional biases in peripersonal space. Participants placed a single hand on a visual display and detected targets appearing near or far from the hand...
May 14, 2018: Consciousness and Cognition
https://www.readbyqxmd.com/read/29773362/regioselective-chlorination-of-cellulose-esters-by-methanesulfonyl-chloride
#20
Chengzhe Gao, Shu Liu, Kevin J Edgar
Regioselective chlorination of cellulose is challenging due to its low reactivity, the small reactivity differences between cellulosic hydroxyl groups, and the high and diverse reactivity of most common chlorinating agents. Halogenation of cellulose affords useful precursors for subsequent nucleophilic substitution reactions, permitting incorporation of new functionality. Herein we report a simple and efficient pathway for preparation of 6-chloro-6-deoxycellulose esters and their derivatives. Cellulose acetate (degree of substitution (DS) 1...
August 1, 2018: Carbohydrate Polymers
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