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https://www.readbyqxmd.com/read/29331918/dna-damage-in-marine-rock-oyster-saccostrea-cucullata-exposed-to-environmentally-available-pahs-and-heavy-metals-along-the-arabian-sea-coast
#1
Subhodeep Sarker, Deepti Vashistha, Munmun Saha Sarker, A Sarkar
Molecular biomarkers are used world wide for quick assessment of the immediate effect of environmental pollution on marine ecosystems. Recently, we evaluated oxidative stress responses of marine rock oyster, Saccostrea cucullata impacted due to polycyclic aromatic hydrocarbons (PAHs) accumulated in their tissues at a few sampling sites along the coast of Goa around the region of the Arabian sea coast, India (Sarkar et al., 2017). Using a combination of partial alkaline unwinding and comet assays, we now report a comprehensive study on the impairment of DNA integrity (DI) in S...
January 11, 2018: Ecotoxicology and Environmental Safety
https://www.readbyqxmd.com/read/29330227/earlier-post-operative-hypocortisolemia-may-predict-durable-remission-from-cushing-s-disease
#2
Natasha Ironside, Gregoire Chatain, David Asuzu, Sarah Benzo, Maya Lodish, Susmeeta Sharma, Lynnette Nieman, Constantine Stratakis, Russell Lonser, Prashant Chittiboina
CONTEXT: Achievement of hypocortisolemia following transsphenoidal surgery (TSS) for Cushing's disease (CD) is associated with successful adenoma resection. However, up to one third of these patients recur. OBJECTIVE: We assessed whether delay in reaching post-operative cortisol nadir may delineate those at risk of recurrence for CD following TSS. METHODS: A retrospective review of of 257 patients who received 291 TSS procedures for CD at NIH, between 2003 and 2016...
January 12, 2018: European Journal of Endocrinology
https://www.readbyqxmd.com/read/29327805/benzonorcorrole-ni-ii-complexes-enhancement-of-paratropic-ring-current-and-singlet-diradical-character-by-benzo-fusion
#3
Takuya Yoshida, Kohtaro Takahashi, Yuki Ide, Ryohei Kishi, Jun-Ya Fujiyoshi, Sangsu Lee, Yuya Hiraoka, Dongho Kim, Masayoshi Nakano, Takahisa Ikeue, Hiroko Yamada, Hiroshi Shinokubo
Fused benzene rings to antiaromatic compounds generally improve their stability but attenuate their antiaromaticity. Here we report the opposite case. We have synthesized Ni(II) benzonorcorroles and elucidated the effect of benzo-fusion on the antiaromaticity. The benzo-fusion resulted in significant decrease of the HOMO-LUMO gaps and enhancement of the paratropic ring current effect. Furthermore, the introduction of the benzo groups induced singlet diradical character in the antiaromaric porphyrinoid.
January 12, 2018: Angewandte Chemie
https://www.readbyqxmd.com/read/29327461/well-balanced-ambipolar-conjugated-polymers-featuring-mild-glass-transition-temperatures-toward-high-performance-flexible-field-effect-transistors
#4
Keli Shi, Weifeng Zhang, Dong Gao, Shiying Zhang, Zuzhang Lin, Ye Zou, Liping Wang, Gui Yu
Conjugated polymers, which can be fabricated by simple processing techniques and possess excellent electrical performance, are key to the fabrication of flexible polymer field-effect transistors (PFETs) and integrated circuits. Herein, two ambipolar conjugated polymers based on (3E,7E)-3,7-bis(2-oxo-1H-pyrrolo[2,3-b]pyridin-3(2H)-ylidene)benzo[1,2-b:4,5-b']difuran-2,6(3H,7H)-dione and dithienylbenzothiadiazole units, namely PNBDOPV-DTBT and PNBDOPV-DTF2BT, are developed. Both copolymers possess almost planar conjugated backbone conformations and suitable highest occupied molecular orbital (HOMO)/lowest unoccupied molecular orbital (LUMO) energy levels (-5...
January 12, 2018: Advanced Materials
https://www.readbyqxmd.com/read/29327456/discovery-and-characterization-of-cd12681-a-potent-ror%C3%AE-inverse-agonist-preclinical-candidate-for-the-topical-treatment-of-psoriasis
#5
Gilles Ouvry, Nicolas Atrux-Tallau, Franck Bihl, Aline Bondu, Claire Bouix-Peter, Isabelle Carlavan, Olivier Christin, Marie-Josée Cuadrado, Claire Defoin-Platel, Sophie Deret, Denis Duvert, Christophe Feret, Mathieu Forissier, Jean-François Fournier, David Froude, Fériel Hacini-Rachinel, Craig Steven Harris, Catherine Hervouet, Hélène Huguet, Guillaume Lafitte, Anne-Pascale Luzy, Branislav Musicki, Danielle Orfila, Benjamin Ozello, Coralie Pascau, Jonathan Pascau, Véronique Parnet, Guillaume Peluchon, Romain Pierre, David Piwnica, Catherine Raffin, Patricia Rossio, Delphine Spiesse, Nathalie Taquet, Etienne Thoreau, Rodolphe Vatinel, Emmanuel Vial, Laurent François Hennequin
With possible implications in multiple autoimmune diseases, the retinoic acid receptor-related orphan receptor RORγ has become a very sought-after target in the pharmaceutical industry. Herein are described the efforts to identify a potent RORγ inverse agonist compatible with topical application for the treatment of skin diseases. These efforts culminated with the discovery of CD12681 (compound 14; N-(2,4-dimethylphenyl)-N-isobutyl-2-oxo-1-((tetrahydro-2H-pyran-4-yl)methyl)-2,3-dihydro-1H-benzo[d]imidazole-5-sulfonamide), a potent inverse agonist with in vivo activity in an IL-23 induced skin inflammation model in mouse...
January 12, 2018: ChemMedChem
https://www.readbyqxmd.com/read/29327141/theoretical-study-on-benzoheterocycle-based-energetic-materials-effect-of-heterocyclic-fused-conjugation-hydrogen-bond-and-substitutional-group-on-the-detonation-performance
#6
Cheng Shen, Pengcheng Wang, Ming Lu
In this paper, four series of benzoheterocycle based energetic materials (EMs) have been designed to plan out a strategy to improve the density and safety of EMs, such as combining the insensitive group with aminobenzene ring and the high energetic nitramine explosives, benzo-heterocycle mother ring, designing multi-nitrogen heterocycles with a conjugated system containing N-N and C-N high energy bonds, and hydrogen bonding. Their optimized structure and detonation properties were first calculated and discussed using DFT methods...
January 11, 2018: Journal of Molecular Modeling
https://www.readbyqxmd.com/read/29324345/synthesis-and-biological-evaluation-of-a-series-of-multi-target-n-substituted-cyclic-imide-derivatives-with-potential-antipsychotic-effect
#7
Mingshuo Xu, Yu Wang, Feipu Yang, Chunhui Wu, Zhen Wang, Bin Ye, Xiangrui Jiang, Qingjie Zhao, Jianfeng Li, Yongjian Liu, Junchi Zhang, Guanghui Tian, Yang He, Jingshan Shen, Hualiang Jiang
In the present study, a series of multi-target N-substituted cyclic imide derivatives which possessed potent dopamine D2, serotonin 5-HT1A and 5-HT2A receptors properties were synthesized and evaluated as potential antipsychotics. Among these compounds, (3aR,4R,7S,7aS)-2-(4-(4-(benzo[b]thiophen-4-yl)piperazin-1-yl)butyl)-3a,4,7,7a-tetrahydro-1H-4,7-methanoisoindole-1,3(2H)-dione hydrochloride (3d) held a promising pharmacological profile. 3d not only showed potent and balanced in vitro activities on D2/5-HT1A/5-HT2A receptors, but also endowed with low to moderate activities on 5-HT2C, H1, α1A, M3 receptors and hERG channel, suggesting a low liability to induce side effects such as weight gain, orthostatic hypotension and QT prolongation...
January 4, 2018: European Journal of Medicinal Chemistry
https://www.readbyqxmd.com/read/29323905/a-palladium-iodide-catalyzed-oxidative-aminocarbonylation-heterocyclization-approach-to-functionalized-benzimidazoimidazoles
#8
Lucia Veltri, Salvatore V Giofrè, Perry Devo, Roberto Romeo, Adrian P Dobbs, Bartolo Gabriele
A novel carbonylative approach to the synthesis of functionalized 1H-benzo[d]imidazo[1,2-a]imidazoles is presented. The method consists in the oxidative aminocarbonylation of N-substituted-1-(prop-2-yn-1-yl)-1H-benzo[d]imidazol-2-amines, carried out in the presence of secondary nucleophilic amines, to give the corresponding alkynylamide intermediates, followed by in situ conjugated addition and double bond isomerization, to give 2-(1-alkyl-1H-benzo[d]imidazo[1,2-a]imidazol-2-yl)acetamides. Products were obtained in good to excellent yields (64-96%) and high turnover numbers (192-288 mol of product per mol of catalyst) under relatively mild conditions (100 °C under 20 atm of a 4:1 mixture of CO-air), using a simple catalytic system, consisting of PdI2 (0...
January 11, 2018: Journal of Organic Chemistry
https://www.readbyqxmd.com/read/29323883/a-stable-blue-photosensitizer-for-color-palette-of-dye-sensitized-solar-cells-reaching-12-6-efficiency
#9
Yameng Ren, Danyang Sun, Yiming祎明 Cao曹, Hoi Nok Tsao, Yi Yuan, Shaik M Zakeeruddin, Peng Wang, Michael Grätzel
We report a blue donor-acceptor organic dye, coded as R6, which features a primary chromophore of a polycyclic aromatic hydrocarbon 9,19-dihydrobenzo[1',10']phenanthro[3',4':4,5]thieno[3,2-b]benzo[1,10]phenanthro[3,4-d]thiophene (BPT2) coupled with a diarylamine electron-donor and 4-(7-ethynylbenzo[c][1,2,5]thiadiazol-4-yl)benzoic acid acceptor. Dye R6 displays a brilliant sapphire color on a sensitized titania mesoporous film together with a Co(II/III)tris(bipyridyl)-based redox electrolyte. Significantly, such judiciously tailored DSCs achieve an impressive solar-to-electric power conversion efficiency (PCE) of 12...
January 11, 2018: Journal of the American Chemical Society
https://www.readbyqxmd.com/read/29320557/high-ahr-expression-in-breast-tumors-correlates-with-expression-of-genes-from-several-signaling-pathways-namely-inflammation-and-endogenous-tryptophan-metabolism
#10
Sophie Vacher, Patrice Castagnet, Walid Chemlali, François Lallemand, Didier Meseure, Marc Pocard, Ivan Bieche, Martine Perrot-Applanat
Increasing epidemiological and animal experimental data provide substantial support for the role of aryl hydrocarbon receptor (AhR) in mammary tumorigenesis. The effects of AhR have been clearly demonstrated in rodent models of breast carcinogenesis and in several established human breast cancer cell lines following exposure to AhR ligands or AhR overexpression. However, relatively little is known about the role of AhR in human breast cancers. AhR has always been considered to be a regulator of toxic and carcinogenic responses to environmental contaminants such as TCDD (dioxin) and benzo[a]pyrene (BaP)...
2018: PloS One
https://www.readbyqxmd.com/read/29320438/modeling-unobserved-heterogeneity-in-susceptibility-to-ambient-benzo-a-pyrene-concentration-among-children-with-allergic-asthma-using-an-unsupervised-learning-algorithm
#11
Daniel Fernández, Radim J Sram, Miroslav Dostal, Anna Pastorkova, Hans Gmuender, Hyunok Choi
Current studies of gene × air pollution interaction typically seek to identify unknown heritability of common complex illnesses arising from variability in the host's susceptibility to environmental pollutants of interest. Accordingly, a single component generalized linear models are often used to model the risk posed by an environmental exposure variable of interest in relation to a priori determined DNA variants. However, reducing the phenotypic heterogeneity may further optimize such approach, primarily represented by the modeled DNA variants...
January 10, 2018: International Journal of Environmental Research and Public Health
https://www.readbyqxmd.com/read/29319090/synthesis-of-functionalized-helical-bn-benzo-c-phenanthrenes
#12
Alberto Abengózar, Patricia García-García, David Sucunza, Adrián Pérez-Redondo, Juan J Vaquero
A novel parent BN-benzo[c]phenanthrene, with helical chirality and remarkable structural features, has been easily obtained in three steps with a global yield of 55%. Moreover, Cl-substituted derivatives have been prepared and these have served as useful starting materials for the development of palladium-catalyzed cross-coupling reactions.
January 10, 2018: Chemical Communications: Chem Comm
https://www.readbyqxmd.com/read/29318676/metal-complex-controlled-regio-diastero-and-enantioselective-1-3-dipolar-cycloaddition-of-azomethine-ylides-with-benzo-b-thiophene-sulfones
#13
Masato Harada, Shuma Kato, Ryosuke Haraguchi, Shin-Ichi Fukuzawa
The Cu(MeCN)4PF6/DTBM-Segphos complex catalyzed the highly diastereo- and enantioselective 1,3-dipolar cycloaddition of azomethine ylides with benzo[b]thiophene sulfones with the usual regiochemistry to give single isomers of the exo-cycloadducts in good yields. In contrast, the AgOAc/ThioClickFerrophos complex catalyzed the reaction with atypical regiochemistry to give the endo-cycloadducts as major products with excellent enantioselectivities. Thus, the choice of chiral metal complex enabled the regio- and stereoselective synthesis of chiral fused sulfolanes...
January 9, 2018: Chemistry: a European Journal
https://www.readbyqxmd.com/read/29318401/synthesis-anti-microbial-activity-cytotoxicity-of-some-novel-substituted-5-3-1h-benzo-d-imidazol-2-yl-4-hydroxybenzyl-benzofuran-2-yl-phenyl-methanone-analogs
#14
Bhookya Shankar, Pochampally Jalapathi, Balabadra Saikrishna, Shaym Perugu, Vijjulatha Manga
BACKGROUND: There is a dire need for the discovery and development of new antimicrobial agents after several experiments for a better resistance of microorganisms towards antimicrobial agents become a serious health problem for a few years in the past. As benzimidazole possess various types of biological activities, it has been synthesized, in the present study, a new series of (5-(3-(1H-benzo[d]imidazol-2-yl)-4-hydroxybenzyl)benzofuran-2-yl)(phenyl)methanone analogs by using the condensation and screened for its in vitro antimicrobial activity and cytotoxicity...
January 9, 2018: Chemistry Central Journal
https://www.readbyqxmd.com/read/29318312/microwave-assisted-one-pot-efficient-synthesis-of-functionalized-2-oxo-2-phenylethylidenes-linked-2-oxobenzo-1-4-oxazines-and-2-oxoquino-1-4-oxalines-synthetic-applications-antioxidant-activity-sar-and-cytotoxic-studies
#15
Vashundhra Sharma, Pradeep K Jaiswal, Dharmendra K Yadav, Mukesh Saran, Jaroslav Prikhodko, Manas Mathur, Ajit K Swami, Irina V Mashevskaya, Sandeep Chaudhary
A microwave-assisted, environmentally benign green protocol for the synthesis of functionalized (Z)-3-(2-oxo-2-phenylethylidene)-3, 4-dihydro-2H-benzo[b][1,4]oxazin-2-ones (11a-n) in excellent yields (upto 97%) and (Z)-3-(2-oxo-2-phenylethylidene)-3,4-dihydroquinoxalin-2(1H)-ones (14a-h) (upto 96% yield) are reported. The practical applicability of developed methodology were also confirmed by the gram scale synthesis of 11a, 14c and 14e; synthesis of anticancer alkaloid Cephalandole A 16 (89% yield). All the synthesized compounds 11a-n, 14a-h and 16 were assessed for their in vitro antioxidant activities in DPPH radical scavenging and FRAP assay...
December 2017: Acta Chimica Slovenica
https://www.readbyqxmd.com/read/29318096/a-two-photon-ratiometric-fluorescent-probe-for-imaging-of-hydrogen-peroxide-levels-in-rat-organ-tissues
#16
Chang Su Lim, Myoung Ki Cho, Mi Yeon Park, Hwan Myung Kim
Hydrogen peroxide (H2O2) is important in the regulation of a variety of biological processes and is involved in various diseases. Quantitative measurement of H2O2 levels at the subcellular level is important for understanding its positive and negative effects on biological processes. Herein, a two-photon ratiometric fluorescent probe (SHP-Cyto) with a boronate-based carbamate leaving group as the H2O2 reactive trigger and 6-(benzo[d]thiazol-2'-yl)-2-(N,N-dimethylamino) naphthalene (BTDAN) as the fluorophore was synthesized and examined for its ability to detect cytosolic H2O2 in situ...
January 2018: ChemistryOpen
https://www.readbyqxmd.com/read/29317668/hygroscopic-coating-of-sulfuric-acid-shields-oxidant-attack-on-the-atmospheric-pollutant-benzo-a-pyrene-bound-to-model-soot-particles
#17
Debajyoti Ray, Tara Shankar Bhattacharya, Abhijit Chatterjee, Achintya Singha, Sanjay K Ghosh, Sibaji Raha
Substantial impacts on climate have been documented for soot‒sulfuric acid (H2SO4) interactions in terms of optical and hygroscopic properties of soot aerosols. However, the influence of H2SO4 on heterogeneous chemistry on soot remains unexplored. Additionally, oxidation rate coefficients for polycyclic aromatic hydrocarbons intrinsic to the atmospheric particles evaluated in laboratory experiments seem to overestimate their degradation in ambient atmosphere, possibly due to matrix effects which are hitherto not mimicked in laboratory experiments...
January 9, 2018: Scientific Reports
https://www.readbyqxmd.com/read/29316740/benzo-a-pyrene-alters-the-expression-of-genes-in-a549-lung-cancer-cells-and-cancer-stem-cells
#18
Yesol Bak, Hui-Joo Jang, Ji-Hye Seo, Su-Hyun No, Jung-Il Chae, Jintae Hong, Do-Young Yoon
Benzo[a]pyrene (B[a]P), a polycyclic aromatic hydrocarbon, is a principal component of cigarette smoke. B[a]P can cause lung carcinogenesis and plays a key role in lung cancer progression. The role of B[a]P has been reported in lung cancer, but its effects on lung cancer stem cells have not been investigated. Emerging evidence indicates that cancer stem cells (CSCs) are associated with carcinogenesis, tumor initiation, relapse, and metastasis. Therefore, targeting CSCs to defeat cancer is a challenging issue in the clinic...
January 11, 2018: Journal of Microbiology and Biotechnology
https://www.readbyqxmd.com/read/29315775/expression-of-aryl-hydrocarbon-receptor-regulated-genes-and-superoxide-dismutase-in-the-antarctic-eelpout-pachycara-brachycephalum-exposed-to-benzo-a-pyrene
#19
Anneli Strobel, Felix C Mark, Helmut Segner, Patricia Burkhardt-Holm
The aryl hydrocarbon receptor (AHR) pathway mediates many, if not all, responses of fish to dioxin-like compounds. The Southern Ocean is progressively exposed to increasing concentrations of anthropogenic pollutants. Antarctic fish are known to accumulate those pollutants, yet nothing is known about their capability to induce chemical biotransformation via the AHR pathway. The objective of this study was to investigate if Antarctic eelpout, Pachycara brachycephalum, respond to anthropogenic pollutants by activation of the AHR and its target gene cytochrome P4501A (CYP1A), and of superoxide dismutase (SOD) which served as a representative for oxidative stress...
January 5, 2018: Environmental Toxicology and Chemistry
https://www.readbyqxmd.com/read/29315592/identification-of-a-pyranocoumarin-photosensitizer-that-is-a-potent-inhibitor-of-keratinocyte-growth
#20
Jeffrey D Laskin, Yi-Hua Jan, Michele M Jetter, Christophe D Guillon, Thomas M Mariano, Diane E Heck, Ned D Heindel
Photosensitizers are used in the treatment of epidermal proliferation and differentiation disorders such as psoriasis and vitiligo. In the present studies, a ring-expanded carbon homologue of the linear psoralen (furo[3,2-g]benzopyran-7-one) class of photosensitizers, 4,10-dimethyl-2H,8H-benzo[1,2-b:5,4-b']dipyran-2-one (NDH2476), was synthesized and analyzed for biological activity. Following activation by ultraviolet light (UVA, 320-400 nm), NDH2476 was found to be a potent inhibitor of keratinocyte growth (IC50 = 9 nM)...
January 6, 2018: Photochemistry and Photobiology
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