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https://www.readbyqxmd.com/read/28342691/indenocinnoline-derivatives-as-g-quadruplex-binders-topoisomerase-ii%C3%AE-inhibitors-and-antiproliferative-agents
#1
Grigoris Zoidis, Alice Sosic, Silvia Da Ros, Barbara Gatto, Claudia Sissi, Fausta Palluotto, Angelo Carotti, Marco Catto
DNA intercalating agents are a consolidated therapeutic option in the treatment of tumor diseases. Starting from previous findings in the antiproliferative efficacy of a series of indeno[1,2-c]cinnoline-11-one derivatives, we performed a suitable decoration of this scaffold by means of a simple and straightforward chemistry, aiming to a) enlarge the planar core to a pentacyclic benzo[h]indeno[1,2-c]cinnoline-13-one and b) introduce a basic head tethered through a simple polymethylene chain. In fluorescence melting and fluorescence intercalator displacement assays, these new compounds displayed fair to very good intercalating properties on different nucleic acid strands, with preference for G-quadruplex sequences...
March 11, 2017: Bioorganic & Medicinal Chemistry
https://www.readbyqxmd.com/read/28340412/discovery-of-2-substituted-1h-benzo-d-immidazole-4-carboxamide-derivatives-as-novel-poly-adp-ribose-polymerase-1-inhibitors-with-in%C3%A2-vivo-anti-tumor-activity
#2
Jie Zhou, Ming Ji, Zhixiang Zhu, Ran Cao, Xiaoguang Chen, Bailing Xu
Novel 1H-benzo[d]immidazole-4-carboxamide derivatives bearing five-membered or six-membered N-heterocyclic moieties at the 2-position were designed and synthesized as PARP-1 inhibitors. Structure-activity relationships were conducted and led to a number of potent PARP-1 inhibitors having IC50 values in the single or double digit nanomolar level. Some potent PARP-1 inhibitors also had similar inhibitory activities against PARP-2. Among all the synthesized compounds, compound 10a and 11e displayed strong potentiation effects on temozolomide (TMZ) in MX-1 cells (PF50 = 7...
March 18, 2017: European Journal of Medicinal Chemistry
https://www.readbyqxmd.com/read/28338331/an-in-silico-study-on-the-isomers-of-pentacene-the-case-for-air-stable-and-alternative-c22h14-acenes-for-organic-electronics
#3
Leighton Jones, Long Lin
Pentacene is one of the most investigated candidates for organic thin film transistor (OTFT) applications over the last few decades even though it unstable in air (Eg = 1.80 eV), owing in part to its planar nature and high charge-transfer mobilities as both a single crystal (35 cm2 V 1 s 1) and as a thin-film (3.0 cm2 V 1 s 1). Until now, picene is the only isomer of pentacene to be investigated for organic electronic applications, due to its greater stability (Eg = 4.21 eV) and high charge transfer mobility (3...
March 24, 2017: Journal of Physical Chemistry. A
https://www.readbyqxmd.com/read/28337918/rh-catalyzed-annulations-of-n-methoxybenzamides-and-ketenimines-steric-and-electronic-controlled-synthesis-of-isoquinolinones-and-isoindolinones
#4
Xiaorong Zhou, Zhiyin Zhang, Hongyang Zhao, Ping Lu, Yanguang Wang
Rhodium-catalyzed C-H activation/annulation reactions of ketenimines with N-methoxybenzamides are reported. The outcome of reactions is dependent on the structure of ketenimines. The β-alkyl-substituted ketenimines furnish 3-iminoisoquinolin-1(2H)-ones through a formal [4+2] annulation manner, while the β-ester substituted ketenimines afford 3-aminoisoindolin-1-ones through a formal [4+1] annulation manner. The synthesized [4+2] products undergo an intramolecular Cu-catalyzed C-N coupling to be converted to benzo[4,5]imidazo[1,2-b]isoquinolin-11-ones, which can be directly prepared from ketenimines and N-methoxybenzamides by a one-pot Rh-catalyzed annulation /Cu-catalyzed C-N coupling sequence...
March 24, 2017: Journal of Organic Chemistry
https://www.readbyqxmd.com/read/28335591/heteroatom-doped-perihexacene-from-a-double-helicene-precursor-on-surface-synthesis-and-properties
#5
Xiao-Ye Wang, Thomas Dienel, Marco Di Giovannantonio, Gabriela Borin Barin, Neerav Kharche, Okan Deniz, José I Urgel, Roland Widmer, Samuel Stolz, Luis Henrique De Lima, Matthias Muntwiler, Matteo Tommasini, Vincent Meunier, Pascal Ruffieux, Xinliang Feng, Roman Fasel, Klaus Müllen, Akimitsu Narita
We report on the surface-assisted synthesis and spectroscopic characterization of the hitherto longest periacene analogue with oxygen-boron-oxygen (OBO) segments along the zigzag edges, that is, a heteroatom-doped perihexacene 1. Surface-catalyzed cyclodehydrogenation successfully transformed the double helicene precursor 2, i.e. 12a,26a-dibora-12,13,26,27-tetraoxa-benzo[1,2,3-hi:4,5,6-h'i']dihexacene, into the planar perihexacene analogue 1, which was visualized by scanning tunneling microscopy (STM) and noncontact atomic force microscopy (nc-AFM)...
March 23, 2017: Journal of the American Chemical Society
https://www.readbyqxmd.com/read/28335470/design-of-new-benzo-h-chromene-derivatives-antitumor-activities-and-structure-activity-relationships-of-the-2-3-positions-and-fused-rings-at-the-2-3-positions
#6
Rawda M Okasha, Fawzia F Alblewi, Tarek H Afifi, Arshi Naqvi, Ahmed M Fouda, Al-Anood M Al-Dies, Ahmed M El-Agrody
A series of novel 4H-benzo[h]chromenes 4, 6-11, 13, 14; 7H-benzo[h]chromeno[2,3-d]pyrimidines 15-18, 20, and 14H-benzo[h]chromeno[3,2-e][1,2,4]triazolo[1,5-c]pyrimidine derivatives 19a-e, 24 was prepared. The structures of the synthesized compounds were characterized on the basis of their spectral data. Some of the target compounds were examined for their antiproliferative activity against three cell lines; breast carcinoma (MCF-7), human colon carcinoma (HCT-116) and hepatocellular carcinoma (HepG-2). The cytotoxic behavior has been tested using MTT assay and the inhibitory activity was referenced to three standard anticancer drugs: vinblastine, colchicine and doxorubicin...
March 18, 2017: Molecules: a Journal of Synthetic Chemistry and Natural Product Chemistry
https://www.readbyqxmd.com/read/28334921/internal-hydrolysis-indicator-for-sample-specific-monitoring-of-%C3%AE-glucuronidase-activity
#7
Lacy L Taylor, Noah A Flint, Vinh Ma, Brandy M Hill, Chantry J Clark, Frederick G Strathmann
Metabolized forms of benzodiazepines (benzos) can cause issues with mass spectrometry identification. Benzodiazepines undergo a process called glucuronidation during metabolism that attaches a glucuronic acid for increased solubility. Often in clinical testing an enzymatic hydrolysis step is implemented to increase the sensitivity of benzodiazepines by hydrolyzing β-D-glucuronic acid from benzodiazepine-glucuronide conjugates in urine samples using the β-Glucuronidase enzyme. In this study resorufin β-D-glucuronide, a substrate of the β-Glucuronidase enzyme, was added to patient samples to determine if proper hydrolysis had occurred...
March 18, 2017: Journal of Analytical Toxicology
https://www.readbyqxmd.com/read/28332845/terrazoanthines-2-aminoimidazole-alkaloids-from-the-tropical-eastern-pacific-zoantharian-terrazoanthus-onoi
#8
Paul O Guillen, Karla B Jaramillo, Gregory Genta-Jouve, Frederic Sinniger, Jenny Rodriguez, Olivier P Thomas
The first chemical study of the common species Terrazoanthus onoi, present off the coast of Ecuador, led to the identification of a new family of 2-aminoimidazole alkaloids named terrazoanthines A-C (1-3). Homologues 1 and 2 feature an unprecedented 6-(imidazol-5-yl)benzo[d]imidazole. Acyl substitution pattern and complete configurational assignments were deduced from comparison between experimental and theoretical (13)C NMR and ECD data, respectively. These compounds may represent key derivatives in the biosynthesis of zoanthoxanthins...
March 23, 2017: Organic Letters
https://www.readbyqxmd.com/read/28332824/indole-substituted-benzothiazoles-and-benzoxazoles-as-selective-and-reversible-mao-b-inhibitors-for-treatment-of-parkinson-s-disease
#9
Min-Ho Nam, Moosung Park, Hyeri Park, Youngjae Kim, Seulki Yoon, Vikram Shahaji Sawant, Ji Won Choi, Jong-Hyun Park, Ki Duk Park, Sun-Joon Min, Changjoon Justin Lee, Hyunah Choo
To develop a novel, selective, and reversible MAO-B inhibitors for safer treatment of Parkinson's disease, benzothiazole and benzoxazole derivatives with indole moiety were designed and synthesized. Most of the synthesized compounds showed inhibitory activities against MAO-B and selectivity over MAO-A. The most active compound was Compound 5b, 6-fluoro-2-(1-methyl-1H-indol-5-yl)benzo[d]thiazole with an IC50 value of 29 nM with no apparent effect on MAO-A activity at 10 M. Based on the reversibility assay, Compound 5b turned out to be a fully reversible with over 95% of recovery of enzyme activity after washout of the compound...
March 23, 2017: ACS Chemical Neuroscience
https://www.readbyqxmd.com/read/28332750/iridium-catalyzed-asymmetric-hydrogenation-of-benzo-b-thiophene-1-1-dioxides
#10
Paolo Tosatti, Andreas Pfaltz
An efficient iridium-catalyzed asymmetric hydrogenation of substituted benzothiophene 1,1-dioxides is described. The use of iridium complexes with chiral pyridyl phosphinite ligands provides access to highly enantiomerically enriched sulfones with substituents at the 2- and 3-position. Sulfones of this type are of interest as core structures of agrochemicals and pharmaceuticals. Moreover, they can be further reduced to chiral 2,3-dihydrobenzothiophenes.
March 23, 2017: Angewandte Chemie
https://www.readbyqxmd.com/read/28332392/palladium-catalyzed-oxidative-annulation-of-ortho-alkenylanilines-and-allenes-an-access-to-benzo-b-azepines
#11
Lisha Wu, Yinfeng Meng, Jamie Ferguson, Lijie Wang, Fanlong Zeng
Palladium-catalyzed oxidative annulation of ortho-alkenyllanilines and allenes to constitute valuable but synthetically challenging benzo[b]azepines has been developed. The procedure, involving of the cleavage of the terminal C(sp2)-H bond of the vinyl moiety and the participation of allenes as two-carbon cycloaddition partner, is attractive in terms of assembly efficiency and environmentally friendliness. The transformation features mild reaction conditions and good functional group tolerance, resulting in a variety of benzo[b]azepines in good to excellent yields...
March 23, 2017: Journal of Organic Chemistry
https://www.readbyqxmd.com/read/28332173/combined-ultrasound-with-fenton-treatment-for-the-degradation-of-carcinogenic-polycyclic-aromatic-hydrocarbons-in-textile-dying-sludge
#12
Jian-Hao Zhang, Hai-Yuan Zou, Xun-An Ning, Mei-Qing Lin, Chang-Min Chen, Tai-Cheng An, Jian Sun
To develop an effective method to remove the toxic and carcinogenic polycyclic aromatic hydrocarbons (CPAHs) from textile dyeing sludge, five CPAHs were selected to investigate the degradation efficiencies using ultrasound combined with Fenton process (US/Fenton). The results showed that the synergistic effect of the US/Fenton process on the degradation of CPAHs in textile dyeing sludge was significant with the synergy degree of 30.4. During the US/Fenton process, low ultrasonic density showed significant advantage in degrading the CPAHs in textile dyeing sludge...
March 22, 2017: Environmental Geochemistry and Health
https://www.readbyqxmd.com/read/28332138/benzo-a-pyrene-exposure-causes-genotoxic-and-biochemical-changes-in-the-midge-larvae-of-chironomus-sancticaroli-strixino-strixino-diptera-chironomidae
#13
M Vicentini, G S Morais, D Rebechi-Baggio, V S Richardi, G S Santos, M M Cestari, M A Navarro-Silva
Benzo(a)pyrene (BaP) is a carcinogenic polycyclic aromatic hydrocarbon, also found in nature due to human activities. BaP adheres to sediments showing toxic effects on benthic organisms, including midge larvae of the family Chironomidae. We tested for toxic effects of benzo(a)pyrene on Chironomus sancticaroli Strixino & Strixino 1981 using biochemical and genotoxic biomarkers, to identify changes in metabolic and antioxidant pathways, besides neurotoxic and DNA damage. Enzyme activity was compared by exposing larvae to four nominal concentrations (0...
March 22, 2017: Neotropical Entomology
https://www.readbyqxmd.com/read/28329817/early-life-benzo-a-pyrene-exposure-causes-neurodegenerative-syndromes-in-adult-zebrafish-danio-rerio-and-the-mechanism-involved
#14
Dongxu Gao, Chonggang Wang, Zhihui Xi, Yixi Zhou, Yuanchuan Wang, Zhenghong Zuo
There is increasing recognition of the importance of early-life environmental exposures in health disorders at later-life stages. The aim of this study was to evaluate whether early-life exposure to benzo[a]pyrene (BaP) could induce neurodegenerative syndromes at later-life stages in zebrafish. Embryos were exposed to BaP at doses of 0, 0.05, 0.5, 5, and 50 nM from early embryogenesis to 96 h post-fertilization (hpf), then transferred to clean water and maintained for 365 days. We found that BaP decreased locomotor and cognitive ability, neurotransmitter levels of dopamine, 3,4-dihydroxyphenylacetic acid and norepinephrine; and induced loss of dopaminergic neurons and resulted in neurodegeneration...
January 30, 2017: Toxicological Sciences: An Official Journal of the Society of Toxicology
https://www.readbyqxmd.com/read/28327162/biological-effects-of-carbon-black-nanoparticles-are-changed-by-surface-coating-with-polycyclic-aromatic-hydrocarbons
#15
Karina Lindner, Michael Ströbele, Sandra Schlick, Sina Webering, André Jenckel, Johannes Kopf, Olga Danov, Katherina Sewald, Christian Buj, Otto Creutzenberg, Thomas Tillmann, Gerhard Pohlmann, Heinrich Ernst, Christina Ziemann, Gereon Hüttmann, Holger Heine, Henning Bockhorn, Tanja Hansen, Peter König, Heinz Fehrenbach
BACKGROUND: Carbon black nanoparticles (CBNP) are mainly composed of carbon, with a small amount of other elements (including hydrogen and oxygen). The toxicity of CBNP has been attributed to their large surface area, and through adsorbing intrinsically toxic substances, such as polycyclic aromatic hydrocarbons (PAH). It is not clear whether a PAH surface coating changes the toxicological properties of CBNP by influencing their physicochemical properties, through the specific toxicity of the surface-bound PAH, or by a combination of both...
March 21, 2017: Particle and Fibre Toxicology
https://www.readbyqxmd.com/read/28325143/synthesis-and-characterization-of-a-new-benzo-indole-derivative-with-apoptotic-activity-against-colon-cancer-cells
#16
Fatemeh Hajiaghaalipou, Fadhil Lafta Faraj, Elham Bagheri, Hamid Khaledi, Hapipah Mohd Ali, Nazia Abdul Majid, Mahmood Ameen Abdulla
BACKGROUND: Colorectal cancer is the third most common form of cancer in both men and women around the world. The chemistry and biological study of heterocyclic compounds have been an interesting area for a long time in pharmaceutical and medicinal chemistry. METHODS: A new synthetic compound, 2-(1,1-Dimethyl-1,3-dihydro-benzo[e]indol-2-ylidene)-3-(2-hydroxy-phenylimino)-propionaldehyde, abbreviated as DBID has been synthesized by reaction of 2-(1,1-Dimethyl-1,3-dihydro-benzo[e]indol-2-ylidene)-malonaldehyde with 2-aminophenol...
March 20, 2017: Current Pharmaceutical Design
https://www.readbyqxmd.com/read/28325086/application-of-bacterial-reverse-mutation-assay-for-detection-of-non-genotoxic-carcinogens
#17
Rewan Kanode, Saurabh Chandra, Sharad Sharma
Non-genotoxic carcinogens may play a significant role in development of cancer. Currently short-term assays for mutagenicity classify genotoxic carcinogens and lack the abilities to detect epigenetic carcinogens. The need to develop an endpoint always remains to recognize potentially carcinogenic agents employing rapid and practical bioassays. For this, the present study utilized TA98 and TA1537 tester strains of Salmonella typhimurium to evaluate four non-genotoxic carcinogenic agents (Coumarin, β-Myrcene, Bis(2-ethylhexyl) phthalate and trans-anethole)...
March 22, 2017: Toxicology Mechanisms and Methods
https://www.readbyqxmd.com/read/28324832/determination-of-the-interconversion-energy-barrier-of-three-novel-pentahelicene-derivative-enantiomers-by-dynamic-high-resolution-liquid-chromatography
#18
Pavel Majek, Jan Krupcik, Zachary S Breitbach, Milan K Dissanayake, Peter Kroll, Aaron A Ruch, LeGrande M Slaughter, Daniel W Armstrong
Dynamic high resolution liquid chromatography (DHPLC) was used to determine the kinetic and thermodynamic activation parameters of interconversion of three novel pentahelicene derivatives {3,5-bis(trifluoromethyl)benzo[i]pentahelicene, naphtho[1,2-i]pentahelicene and 4-methoxybenzo[i]pentahelicene}. DHPLC was performed on a chiral isopropyl - carbamate cyclofructan 6 (LARIHC CF6-P) column under normal phase conditions. Variation of the column temperature and flow rate was used to study the interconversion process...
December 21, 2016: Journal of Chromatography. B, Analytical Technologies in the Biomedical and Life Sciences
https://www.readbyqxmd.com/read/28323961/normalized-early-post-operative-cortisol-and-acth-values-predict-nonremission-after-surgery-for-cushing-s-disease
#19
David Asuzu, Grégoire P Chatain, Christina Hayes, Sarah Benzo, Raven McGlotten, Meg Keil, Andrea Beri, Susmeeta T Sharma, Lynnette Nieman, Maya Lodish, Constantine Stratakis, Russell R Lonser, Edward H Oldfield, Prashant Chittiboina
Context: Perioperative increases in adrenocorticotropic hormone (ACTH) and cortisol mimic corticotropin releasing hormone (CRH) stimulation testing. This phenomenon may help identify patients with residual adenoma after transsphenoidal surgery (TSS) for Cushing's disease (CD). Objective: To predict non-remission after TSS for CD. Design: Retrospective case control study of patients treated at a single center from December 2003 till July 2016...
March 15, 2017: Journal of Clinical Endocrinology and Metabolism
https://www.readbyqxmd.com/read/28319714/occupational-exposure-of-firefighters-to-polycyclic-aromatic-hydrocarbons-in-non-fire-work-environments
#20
Marta Oliveira, Klara Slezakova, Adília Fernandes, João Paulo Teixeira, Cristina Delerue-Matos, Maria do Carmo Pereira, Simone Morais
This work aims to characterize personal exposure of firefighters to polycyclic aromatic hydrocarbons (PAHs) in non-fire work environments (fire stations), and assesses the respective risks. Eighteen PAHs (16 considered by USEPA as priority pollutants, dibenzo[a,l]pyrene and benzo[j]fluoranthene) were monitored in breathing zones of workers at five Portuguese fire stations during a normal shift. The obtained levels of PAHs fulfilled all existent occupational exposure limits as well as air quality guidelines with total concentrations (ΣPAHs) in range of 46...
March 16, 2017: Science of the Total Environment
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