keyword
MENU ▼
Read by QxMD icon Read
search

benzo

keyword
https://www.readbyqxmd.com/read/28092111/design-and-synthesis-of-5-substituted-benzo-d-1-3-dioxole-derivatives-as-potent-anticonvulsant-agents
#1
Shiyang Dong, Tiantian Wang, Chundi Hu, Xiaodong Chen, Yi Jin, Zengtao Wang
A series of 5-substituted benzo[d][1,3]dioxole derivatives was designed, synthesized, and tested for anticonvulsant activity using the maximal electroshock (MES) and subcutaneous pentylenetetrazole (scPTZ) screens. Neurotoxicity was determined by rotarod test. In the preliminary screening, six compounds, 3a, 3c, 3d, and 4d-f, showed promising anticonvulsant activities in the MES model, and compounds 4c and 4d exhibited full protection against seizures at doses of 300 mg/kg in the scPTZ model. Among the synthesized compounds, 3c as the most active compound showed high protection against the MES-induced seizures with an ED50 value of 9...
January 16, 2017: Archiv der Pharmazie
https://www.readbyqxmd.com/read/28090775/reaction-of-push-pull-enaminoketones-and-in-situ-generated-ortho-quinone-methides-synthesis-of-3-acyl-4h-chromenes-and-2-acyl-1h-benzo-f-chromenes-as-precursors-for-hydroxybenzylated-heterocycles
#2
Anton Vladimirovich Lukashenko, Vitaly Aleksandrovich Osyanin, Dmitry Vladimirovich Osipov, Yuri N Klimochkin
A simple and efficient method for the synthesis of 4H-chromenes and 1H-benzo[f]chromenes containing trifluoroacetyl or aroyl group in pyran ring from o-quinone methide precursors and push-pull enaminoketones has been developed. The chromenes are presumably formed through an initial oxa-Diels-Alder reaction followed by an elimination of amine. Possibility of further transformations of given chromenes to o-hydroxybenzylated pyrazoles, isoxazoles and pyridines has been demonstrated.
January 16, 2017: Journal of Organic Chemistry
https://www.readbyqxmd.com/read/28090614/synthesis-and-anticancer-activity-of-benzoselenophene-and-heteroaromatic-derivatives-of-1-2-9-9a-tetrahydrocyclopropa-c-benzo-e-indol-4-one-cbi
#3
Amol B Mhetre, Hangeun Lee, Heekyoung Yang, Kyoungmin Lee, Do-Hyun Nam, Dongyeol Lim
The current study reports the synthesis of different derivatives of benzoselenophene analogs as well as a diverse series of compounds (14a-p, 15 and 16) from 1,2,9,9a-tetrahydrocyclopropa[c]benzo[e]indol-4-one (CBI) and benzoselenophene or heteroaromatic acids. The overall yield of scaffold 12 was improved by an one-pot reaction, which helps in large-scale synthesis of CBI, a duocarmycin alkylation subunit analog. The series of compounds were evaluated for their cytotoxicity against SK-OV3 ovarian cancer cell lines, which revealed that benzoselenophene can enhance or maintain the anticancer activity of the duocarmycin analog upon replacing the indole moiety...
January 16, 2017: Organic & Biomolecular Chemistry
https://www.readbyqxmd.com/read/28088583/environmental-carcinogenesis-and-ph-homeostasis-not-only-a-matter-of-dysregulated-metabolism
#4
REVIEW
Kévin Hardonniere, Laurence Huc, Odile Sergent, Jørn A Holme, Dominique Lagadic-Gossmann
According to the World Health Organization, around 20% of all cancers would be due to environmental factors. Among these factors, several chemicals are indeed well recognized carcinogens. The widespread contaminant benzo[a]pyrene (B[a]P), an often used model carcinogen of the polycyclic aromatic hydrocarbons' family, has been suggested to target most, if not all, cancer hallmarks described by Hanahan and Weinberg. It is classified as a group I carcinogen by the International Agency for Research on Cancer; however, the precise intracellular mechanisms underlying its carcinogenic properties remain yet to be thoroughly defined...
January 11, 2017: Seminars in Cancer Biology
https://www.readbyqxmd.com/read/28078713/the-novel-mtor-complex-1-2-inhibitor-p529-inhibits-human-lung-myofibroblast-differentiation
#5
Keith T Ferguson, Elizabeth E Torr, Ksenija Bernau, Jonathan Leet, Davis Sherris, Nathan Sandbo
Idiopathic pulmonary fibrosis is a progressive and deadly disorder with very few therapeutic options. Palomid 529 (8-(1-hydroxyethyl)-2-methoxy-3-(4-methoxybenzyloxy)-benzo[c]chromen-6-one; P529) is a novel dual inhibitor of mechanistic target of rapamycin complex 1/2 (mTORC1/2). In these studies, we investigated the effect of P529 on TGF-β-dependent signaling and myofibroblast differentiation. TGF-β-induced phosphorylation of the mTORC1 targets, p70 S6 kinase 1 (S6K1) and eukaryotic translation initiation factor 4E binding protein 1 (4E-BP1), were both dose dependently inhibited by P529 in human lung fibroblasts with maximal inhibition occurring between 10-20 µM...
January 11, 2017: Journal of Cellular Biochemistry
https://www.readbyqxmd.com/read/28078483/theoretical-characterization-on-photoelectric-properties-of-benzothiadiazole-and-fluorene-based-small-molecule-acceptor-materials-for-the-organic-photovoltaics
#6
Mingyue Sui, Shuangbao Li, Qingqing Pan, Guangyan Sun, Yun Geng
The upper efficiency of heterojunction organic photovoltaics depends on the increased open-circuit voltage (V oc) and short-circuit current (J sc). So, a higher lowest unoccupied molecular orbital (LUMO) level is necessary for organic acceptor material to possess higher V oc and more photons absorbsorption in the solar spectrum is needed for larger J sc. In this article, we theoretically designed some small molecule acceptors (2∼5) based on fluorene (F), benzothiadiazole, and cyano group (CN) referring to the reported acceptor material 2-[{7-(9,9-di-n-propyl-9H-fluoren-2-yl)benzo[c][1,2,5]thiadiazol-4-yl}methylene]malononitrile (1), the crucial parameters affecting photoelectrical properties of compounds 2∼5 were evaluated by the density functional theory (DFT) and time dependent density functional theory (TDDFT) methods...
January 2017: Journal of Molecular Modeling
https://www.readbyqxmd.com/read/28075605/pyrazolofluostatins-a-c-pyrazole-fused-benzo-a-fluorenes-from-south-china-sea-derived-micromonospora-rosaria-scsio-n160
#7
Wenjun Zhang, Chunfang Yang, Chunshuai Huang, Liping Zhang, Haibo Zhang, Qingbo Zhang, Cheng-Shan Yuan, Yiguang Zhu, Changsheng Zhang
Pyrazolofluostatins A-C (1-3), three new benzo[a]fluorenes with an unprecedented carbon skeleton, were obtained from the South China Sea-derived Micromonospora rosaria SCSIO N160. Their structures were elucidated by extensive spectroscopic analyses. The structure of pyrazolofluostatin A (1) was confirmed by X-ray crystallographic analysis. Notably, 1-3 possessed a benzo[cd]indeno[2,1-f]indazol skeleton with a pyrazole-fused 6/5/6/6/5 pentacyclic ring system. Pyrazolofluostatin A (1) showed moderate antioxidation activity (EC50 48...
January 11, 2017: Organic Letters
https://www.readbyqxmd.com/read/28075505/terminal-uranium-v-vi-nitride-activation-of-carbon-dioxide-and-disulfide-factors-governing-diverse-and-well-defined-cleavage-and-redox-reactions
#8
Stephen Liddle, Peter Cleaves, Christos Kefalidis, Benedict Gardner, Floriana Tuna, Eric McInnes, William Lewis, Laurent Maron
We report the reactivity of terminal uranium(V/VI)-nitrides with CE2 (E = O, S), where we observe well-defined C=E cleavage followed by zero-, one-, and two-electron redox events. The uranium(V)-nitride [U(TrenTIPS)(N)][K(B15C5)2] [1, TrenTIPS = N(CH2CH2NSiPri3)3; B15C5 = benzo-15-crown-5] reacts with CO2 to give [U(TrenTIPS)(O)(NCO)][K(B15C5)2] (3), whereas the uranium(VI)-nitride [U(TrenTIPS)(N)] (2) reacts with CO2 to give isolable [U(TrenTIPS)(O)(NCO)] (4); complex 4 rapidly decomposes to known [U(TrenTIPS)(O)] (5) with concomitant formation of N2 and CO proposed, with the latter trapped as a vanadocene adduct...
January 11, 2017: Chemistry: a European Journal
https://www.readbyqxmd.com/read/28074206/synthesis-reactivity-and-characterization-of-pt-ii-complexes-with-n-n-chelating-ligands-structure-and-dimethylsulfoxide-reactivity-relationship
#9
Konstantinos Ypsilantis, Theodoros Tsolis, Andreas Kourtellaris, Manolis J Manos, John C Plakatouras, Achilleas Garoufis
Platinum(ii) complexes of the formula PtLCl2 [L = 2-(2'-pyridyl)quinoxaline, (pqx) (1), 2,(2'-pyridyl)benzo[g]quinoxaline, (pbqx) (3) and 2,(2'-pyridyl)quinoline, (pqn) (5)] were synthesized and characterized by spectroscopic and X-ray diffraction methods. Also, monodentate coordination of the ligands pqx and pbqx formed the complexes trans-Pt(DMSO)pqxCl2 (2) and trans-Pt(DMSO)pbqxCl2 (4) as it is indicated from X-ray crystal structure and NMR studies. The reaction of the complexes (1), (3) and (5) with DMSO-d6 revealed a ligand-release solvolysis, which was studied by means of NMR techniques...
January 11, 2017: Dalton Transactions: An International Journal of Inorganic Chemistry
https://www.readbyqxmd.com/read/28070576/regio-selective-synthesis-of-diversely-substituted-benzo-a-carbazoles-through-rh-iii-catalyzed-annulation-of-2-arylindoles-with-%C3%AE-diazo-carbonyl-compounds
#10
Bin Li, Beibei Zhang, Xinying Zhang, Xuesen Fan
A novel synthetic approach toward benzo[a]carbazoles or 6-amino benzo[a]carbazoles containing an unprotected NH unit through Rh(iii)-catalyzed cascade reactions of 2-arylindoles or 2-arylindole-3-carbonitriles with α-diazo carbonyl compounds has been established. To our knowledge, this is the first example in which the NH unit of indole is used as a directing group for an intramolecular C(sp(2))-H bond functionalization to give benzo[a]carbazole derivatives. Notably, this method features easily obtainable substrates, good functional group tolerance, excellent regio-selectivity, and high atom-efficiency...
January 10, 2017: Chemical Communications: Chem Comm
https://www.readbyqxmd.com/read/28069128/on-line-mspd-spe-hplc-fld-analysis-of-polycyclic-aromatic-hydrocarbons-in-bovine-tissues
#11
Tania M Gutiérrez-Valencia, Martha P García de Llasera
A fast method was optimized and validated for simultaneous trace determination of four polycyclic aromatic hydrocarbons: benzo[a]anthracene, benzo[b]fluoranthene, benzo[k]fluoranthene and benzo[a]pyrene in bovine tissues. The determination was performed by matrix solid-phase dispersion (MSPD) coupled on-line to solid phase extraction (SPE) and high performance liquid chromatography (HPLC) with fluorescence detection (FLD). The sample was dispersed on C18 silica sorbent and then the on-line MSPD-SPE-HPLC/FLD method was applied...
May 15, 2017: Food Chemistry
https://www.readbyqxmd.com/read/28065544/solar-radiation-as-a-swift-pathway-for-pah-photodegradation-a-field-study
#12
Montse Marquès, Montse Mari, Jordi Sierra, Martí Nadal, José L Domingo
The photodegradation of polycyclic aromatic hydrocarbons (PAHs) may be an important degradation pathway of PAHs in regions with a high solar radiation. The present investigation was aimed at studying the photodegradation of PAHs after their deposition on surface soils with different textures. Photodegradation by-products were also identified and semi-quantified, as well as correlated with the decrease of parent compounds. The experiment was performed by deploying soil samples spiked with a mixture of the 16 US EPA priority PAHs in a methacrylate box, exposed to solar radiation for 7days, meaning a solar energy of 102...
January 5, 2017: Science of the Total Environment
https://www.readbyqxmd.com/read/28065385/processing-of-the-abasic-sites-clustered-with-the-benzo-a-pyrene-adducts-by-the-base-excision-repair-enzymes
#13
Lidia V Starostenko, Nadejda I Rechkunova, Natalia A Lebedeva, Alexander A Lomzov, Vladimir V Koval, Olga I Lavrik
The major enzyme in eukaryotic cells that catalyzes the cleavage of apurinic/apyrimidinic (AP or abasic) sites is AP endonuclease 1 (APE1) that cleaves the phosphodiester bond on the 5'-side of AP sites. We found that the efficiency of AP site cleavage by APE1 was affected by the benzo[a]pyrenyl-DNA adduct (BPDE-dG) in the opposite strand. AP sites directly opposite of the modified dG or shifted toward the 5' direction were hydrolyzed by APE1 with an efficiency moderately lower than the AP site in the control DNA duplex, whereas AP sites shifted toward the 3' direction were hydrolyzed significantly less efficiently...
December 27, 2016: DNA Repair
https://www.readbyqxmd.com/read/28063314/construction-of-pah-degrading-mixed-microbial-consortia-by-induced-selection-in-soil
#14
German Zafra, Ángel E Absalón, Miguel Ángel Anducho-Reyes, Francisco J Fernandez, Diana V Cortés-Espinosa
Bioremediation of polycyclic aromatic hydrocarbons (PAHs)-contaminated soils through the biostimulation and bioaugmentation processes can be a strategy for the clean-up of oil spills and environmental accidents. In this work, an induced microbial selection method using PAH-polluted soils was successfully used to construct two microbial consortia exhibiting high degradation levels of low and high molecular weight PAHs. Six fungal and seven bacterial native strains were used to construct mixed consortia with the ability to tolerate high amounts of phenanthrene (Phe), pyrene (Pyr) and benzo(a)pyrene (BaP) and utilize these compounds as a sole carbon source...
December 21, 2016: Chemosphere
https://www.readbyqxmd.com/read/28063270/identification-and-analytical-characterization-of-six-synthetic-cannabinoids-nnl-3-5%C3%A2-f-npb-22-7%C3%A2-n-5%C3%A2-f-akb-48-7%C3%A2-n-5%C3%A2-f-edmb-pinaca-emb-fubinaca-and-eg-018
#15
Cuimei Liu, Wei Jia, Zhendong Hua, Zhenhua Qian
Clinical and forensic toxicology laboratories are continuously confronted by analytical challenges when dealing with the new psychoactive substances phenomenon. The number of synthetic cannabinoids, the chemical diversity, and the speed of emergence make this group of compounds particularly challenging in terms of detection, monitoring, and responding. Three indazole 7 N positional isomer synthetic cannabinoids, two ethyl 2-amino-3-methylbutanoate-type synthetic cannabinoids, and one 9H-carbazole substituted synthetic cannabinoid were identified in seized materials...
January 7, 2017: Drug Testing and Analysis
https://www.readbyqxmd.com/read/28063149/modulation-of-benzo-a-pyrene-induced-anxiolytic-like-behavior-by-retinoic-acid-in-zebrafish-involvement-of-oxidative-stress-and-antioxidant-defense-system
#16
Ratnalipi Mohanty, Saroj Kumar Das, Manorama Patri
Benzo[a]pyrene (B[a]P) is commonly associated with oxidative stress-induced neurotoxicity. Retinoic acid (RA) has been shown to exhibit neuroprotection in brain, and disruption of RA signaling via excess or deficient RA can lead to oxidative stress. B[a]P contamination in aquatic environment has been shown to lower the internal RA level. Thus, the present study was conducted in wild-type zebrafish to ameliorate the neurotoxic effect of B[a]P by waterborne RA co-supplementation. Findings showed that B[a]P induced anxiolytic-like behavioral response, and altered antioxidant activity in zebrafish is attenuated by RA...
January 6, 2017: Neurotoxicity Research
https://www.readbyqxmd.com/read/28061388/ancestral-benzo-a-pyrene-exposure-affects-bone-integrity-in-f3-adult-fish-oryzias-latipes
#17
Frauke Seemann, Chang-Bum Jeong, Ge Zhang, Miles Teng Wan, Baosheng Guo, Drew Ryan Peterson, Jae-Seong Lee, Doris Wai-Ting Au
Benzo[a]pyrene (BaP) at an environmentally relevant concentration (1μg/L) has previously been shown to affect bone development in a transgenerational manner in F3 medaka (Oryzias latipes) larvae (17dph). Here, we provide novel histomorphometric data demonstrating that the impaired bone formation at an early life stage is not recoverable and can result in a persistent transgenerational impairment of bone metabolism in F3 adult fish. A decrease in bone thickness and the occurrence of microcracks in ancestrally BaP-treated adult male fish (F3) were revealed by MicroCt measurement and histopathological analysis...
December 23, 2016: Aquatic Toxicology
https://www.readbyqxmd.com/read/28059605/fetal-dna-hypermethylation-in-tight-junction-pathway-is-associated-with-neural-tube-defects-a-genome-wide-dna-methylation-analysis
#18
Linlin Wang, Shanshan Lin, Ji Zhang, Tian Tian, Lei Jin, Aiguo Ren
Neural tube defects (NTDs) are a spectrum of severe congenital malformations of fusion failure of the neural tube during early embryogenesis. Evidence on aberrant DNA methylation in NTD development remains scarce, especially when exposure to environmental pollutant is taken into consideration. DNA methylation profiling was quantified using the Infinium HumanMethylation450 array in neural tissues from 10 NTD cases and 8 non-malformed controls (stage 1). Subsequent validation was performed using a Sequenom MassARRAY system in neural tissues from 20 NTD cases and 20 non-malformed controls (stage 2)...
January 6, 2017: Epigenetics: Official Journal of the DNA Methylation Society
https://www.readbyqxmd.com/read/28055196/discovery-of-novel-phosphodiesterase-2a-inhibitors-by-structure-based-virtual-screening-structural-optimization-and-bioassay
#19
Chen Zhang, Ling-Jun Feng, Yiyou Huang, Deyan Wu, Zhe Li, Qian Zhou, Yinuo Wu, Hai-Bin Luo
Phosphodiesterase-2A (PDE2A) is a potential therapeutic target for treatment of Alzheimer's disease and pulmonary hypertension. However, most of the current PDE2A inhibitors have moderate selectivity over other PDEs. In the present study, we described the discovery of novel PDE2A inhibitors by structure-based virtual screening combining pharmacophore model screening, molecular docking, molecular dynamics simulations, and bioassay validation. Nine hits out of 30 molecules from the SPECS database (a hit rate of 30%) inhibited PDE2A with affinity less than 50 μM...
January 18, 2017: Journal of Chemical Information and Modeling
https://www.readbyqxmd.com/read/28049919/utility-of-pyrazolylchalcone-synthon-to-synthesize-azolopyrimidines-under-grindstone-technology
#20
Maher Abd El-Aziz El-Hashash, Sobhi Mohamed Gomha, Elham Ezz El-Arab
A series of pyrazolyl-triazolo[1,5-a]pyrimidines, pyrazolyl-tetrazolo[1,5-a]pyrimidines, pyrazolyl-benzo[4,5]imidazo[1,2-a]pyrimidines and bis-azolopyrimidines were prepared by reaction of pyrazolyl-chalcones or its bis-pyrazolyl-chalcones with the appropriate heterocyclic amines as aminotriazole, aminotetrazole, 2-aminobenzimidazole and 4,6-dimethyl-1H-pyrazolo[3,4-b]pyridin-3-amine by grinding method. The newly synthesized compounds have been characterized on the basis of elemental analysis and spectral data (IR, (1)H- and (13)C-NMR, Mass)...
2017: Chemical & Pharmaceutical Bulletin
keyword
keyword
46080
1
2
Fetch more papers »
Fetching more papers... Fetching...
Read by QxMD. Sign in or create an account to discover new knowledge that matter to you.
Remove bar
Read by QxMD icon Read
×

Search Tips

Use Boolean operators: AND/OR

diabetic AND foot
diabetes OR diabetic

Exclude a word using the 'minus' sign

Virchow -triad

Use Parentheses

water AND (cup OR glass)

Add an asterisk (*) at end of a word to include word stems

Neuro* will search for Neurology, Neuroscientist, Neurological, and so on

Use quotes to search for an exact phrase

"primary prevention of cancer"
(heart or cardiac or cardio*) AND arrest -"American Heart Association"