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https://www.readbyqxmd.com/read/28092860/design-synthesis-and-biological-evaluation-of-quinazoline-phosphoramidate-mustard-conjugates-as-anticancer-drugs
#1
Songwen Lin, Yingbo Li, Yufen Zheng, Laichun Luo, Qi Sun, Zemei Ge, Tieming Cheng, Runtao Li
A series of novel compounds with phosphoramide mustard functionality incorporated into the quinazoline scaffold of EGFR/HER2 inhibitors were designed and synthesized as multi-target-directed ligands against tumor cells. In vitro assays showed that tumor cell lines with high HER2 level were more sensitive to the compounds than tumor cells with low HER2 level. Compound 10d (EMB-3) was one of the most potent inhibitors with IC50 of 7.4 nM and 82 nM against EGFR and HER2, respectively. The mechanism studies were also supported by the effect of 10d-induced DNA damage in MDA-MB-468 cells...
January 3, 2017: European Journal of Medicinal Chemistry
https://www.readbyqxmd.com/read/28092859/n-2-arylmethylimino-ethyl-7-chloroquinolin-4-amine-derivatives-synthesized-by-thermal-and-ultrasonic-means-are-endowed-with-anti-zika-virus-activity
#2
Giselle Barbosa-Lima, Ligia S da Silveira Pinto, Carlos R Kaiser, James L Wardell, Caroline S De Freitas, Yasmine R Vieira, Andressa Marttorelli, José Cerbino Neto, Patrícia T Bozza, Solange M S V Wardell, Marcus V N de Souza, Thiago M L Souza
Zika virus (ZIKV), an emerging Flavivirus, was recently associated with severe neurological complications and congenital diseases. Therefore, development of antiviral agents capable of inhibiting ZIKV replication is urgent. Chloroquine is a molecule with a confirmed safety history for use with pregnant women, and has been found to exhibit anti-ZIKV activity at concentrations around 10 μM. This suggests that modifications to the chloroquine structure could be promising for obtaining more effective anti-ZIKV agents...
January 6, 2017: European Journal of Medicinal Chemistry
https://www.readbyqxmd.com/read/28092858/the-synthesis-and-antistaphylococcal-activity-of-9-13-disubstituted-berberine-derivatives
#3
Jing Wang, Teng Yang, Huang Chen, Yun-Nan Xu, Li-Fang Yu, Ting Liu, Jie Tang, Zhengfang Yi, Cai-Guang Yang, Wei Xue, Fan Yang
A series of novel 9, 13-disubstituted berberine derivatives have been synthesized and evaluated for the antibacterial activities against Staphylococcus aureus, including Newman strain and multidrug-resistant strains (NRS-1, NRS-70, NRS-100, NRS-108, and NRS-271). Compound 20 shows the most potent activity against the growth of Newman strain, with a MIC value of 0.78 μg/mL, which is comparable with the positive control vancomycin. In addition, compound 20, 21, and 33 are highly antistaphylococcal active against five strains of multidrug-resistant S...
January 9, 2017: European Journal of Medicinal Chemistry
https://www.readbyqxmd.com/read/28092849/magnesium-and-manganese-affect-photosynthesis-essential-oil-composition-and-phenolic-compounds-of-tanacetum-parthenium
#4
Soudeh Farzadfar, Fatemeh Zarinkamar, Mostafa Hojati
The accumulation of plant defense metabolites is closely associated with the concentration of nutrient elements, yet data related to the interactive effects of two nutrients on the deployment of phenolics and terpenoids are scare. In the present study, the interaction between magnesium (Mg) and manganese (Mn) on nutrient uptake, photosynthesis, oxidative status and the accumulation of phenolics and terpenoids in the leaves of feverfew plants grown at different concentrations of Mg and Mn was investigated. Nutrient uptake and photosynthesis were associated with the amount of applied Mg but could be modified by the concentration of Mn...
January 3, 2017: Plant Physiology and Biochemistry: PPB
https://www.readbyqxmd.com/read/28092830/trpv1-antagonism-by-piperazinyl-aryl-compounds-a-topomer-comfa-study-and-its-use-in-virtual-screening-for-identification-of-novel-antagonists
#5
Rajendra Kristam, Shashidhar N Rao, Anne Sudha D'Cruz, Vijayalakshmi Mahadevan, Vellarkad N Viswanadhan
Transient Receptor Potential Vanilloid, member 1 (TRPV1), is a non-selective cation channel belonging to the transient receptor potential (TRP) family of ion channels. It occurs in the peripheral and central nervous system, activated by a variety of exogenous and endogenous stimuli, thus playing a key role in transmission of pain. This has been a target for chronic pain since more than a decade and a number of antagonists that progressed into clinical trials have failed due to the unexpected side effect of core body temperature rise, thus halting progress in this field...
January 7, 2017: Journal of Molecular Graphics & Modelling
https://www.readbyqxmd.com/read/28092827/conjugated-polymer-with-carboxylate-groups-hg-2-system-as-a-turn-on-fluorescence-probe-for-label-free-detection-of-cysteine-containing-compounds
#6
Hongyu Mi, Mingming Guan, Jilin Liu, Hongyan Shan, Qiang Fei, Yanfu Huan, Guodong Feng
In this work, a turn on fluorescent sensor, based on Hg(2+) coordination conjugated polymer, was developed to detect cysteine-containing compounds. The fluorescence of conjugated polymer (poly(2,5-bis (sodium 4-oxybutyrate) -1,4 - phenylethynylene-alt-1,4-phenyleneethynylene; PPE-OBS) would be quenched by Hg(2+) because of the coordination-induced aggregation and electron transfers of PPE-OBS toward Hg(2+). When there were some cysteine-containing compounds in PPE-OBS-Hg(2+) system, the fluorescence of PPE-OBS would be recovered...
January 13, 2017: Spectrochimica Acta. Part A, Molecular and Biomolecular Spectroscopy
https://www.readbyqxmd.com/read/28092826/synthesis-ph-dependent-photometric-and-electrochemical-investigation-redox-mechanism-and-biological-applications-of-novel-schiff-base-and-its-metallic-derivatives
#7
Abdur Rauf, Afzal Shah, Abdul Aziz Khan, Aamir Hassan Shah, Rashda Abbasi, Irfan Zia Qureshi, Saqib Ali
A novel Schiff base, 1-((2, 4-dimethylphenylimino)methyl)naphthalen-2-ol abbreviated as (HL) and its four metallic complexes were synthesized and confirmed by (1)H and (13)C NMR, FTIR, TGA and UV-Visible spectroscopy. Schiff base was also characterized by X-ray analysis. The photometric and electrochemical responses of all the synthesized compounds were investigated in a wide pH range. Structures of the compounds were optimized computationally for the evaluation of different physico-chemical parameters. On the basis of electrochemical results the redox mechanistic pathways of the compounds were proposed...
January 9, 2017: Spectrochimica Acta. Part A, Molecular and Biomolecular Spectroscopy
https://www.readbyqxmd.com/read/28092677/wnt-%C3%AE-catenin-signaling-regulates-mitochondrial-activity-to-alter-the-oncogenic-potential-of-melanoma-in-a-pten-dependent-manner
#8
K Brown, P Yang, D Salvador, R Kulikauskas, H Ruohola-Baker, A M Robitaille, A J Chien, R T Moon, V Sherwood
Aberrant regulation of WNT/β-catenin signaling has a crucial role in the onset and progression of cancers, where the effects are not always predictable depending on tumor context. In melanoma, for example, models of the disease predict differing effects of the WNT/β-catenin pathway on metastatic progression. Understanding the processes that underpin the highly context-dependent nature of WNT/β-catenin signaling in tumors is essential to achieve maximal therapeutic benefit from WNT inhibitory compounds. In this study, we have found that expression of the tumor suppressor, phosphatase and tensin homolog deleted on chromosome 10 (PTEN), alters the invasive potential of melanoma cells in response to WNT/β-catenin signaling, correlating with differing metabolic profiles...
January 16, 2017: Oncogene
https://www.readbyqxmd.com/read/28092530/feasibility-of-multi-plane-transmit-beamforming-for-real-time-volumetric-cardiac-imaging-a-simulation-study
#9
Yinran Chen, Ling Tong, Alejandra Ortega, Jianwen Luo, Jan D'hooge
Today's three-dimensional (3-D) cardiac ultrasound imaging systems suffer from relatively low spatial and temporal resolution, limiting their applicability in daily clinical practice. To address this problem, 3-D diverging wave imaging with spatial coherent compounding (DWC) as well as 3-D multi-line-transmit (MLT) imaging have recently been proposed. Currently, the former improves the temporal resolution significantly at the expense of image quality and the risk of introducing motion artifacts whereas the latter only provides a moderate gain in volume rate but mostly preserves quality...
January 10, 2017: IEEE Transactions on Ultrasonics, Ferroelectrics, and Frequency Control
https://www.readbyqxmd.com/read/28092474/novel-histone-deacetylase-6-hdac6-selective-inhibitors-a-patent-evaluation-wo2014181137
#10
Claudia A Simões-Pires, Philippe Bertrand, Muriel Cuendet
The invention described in this patent (WO2014181137) is related to hydroxamic acid derivatives with inhibitory activity towards histone deacetylases (HDACs), their synthetic process and pharmaceutical formulations, as well as a method for treating patients suffering from a list of selected tumoral, inflammatory, cardiac and chronic disorders. HDACs are known to deacetylate histones and other proteins, which makes HDAC inhibitors able to affect cell survival, cell signaling, transport, and gene expression. Those effects have been associated to the therapeutic success of HDAC inhibitors...
January 16, 2017: Expert Opinion on Therapeutic Patents
https://www.readbyqxmd.com/read/28092469/investigational-drugs-in-recent-clinical-trials-for-treatment-resistant-depression
#11
Ricardo P Garay, Carlos A Zarate, Thomas Charpeaud, Leslie Citrome, Christoph U Correll, Ahcène Hameg, Pierre-Michel Llorca
The authors describe the medications for treatment-resistant depression (TRD) in phase II/III of clinical development in the EU and US and provide an opinion on how current treatment can be improved in the near future. Areas covered: Sixty-two trials were identified in US and EU clinical trial registries that included six investigational compounds in recent phase III development and 12 others in recent phase II clinical trials. Glutamatergic agents have been the focus of many studies. A single intravenous dose of the glutamatergic modulator ketamine produces a robust and rapid antidepressant effect in persons with TRD; this effect continues to remain significant for 1 week...
January 16, 2017: Expert Review of Neurotherapeutics
https://www.readbyqxmd.com/read/28092423/-1-h-qnmr-quantification-of-annonaceous-acetogenins-in-crude-extracts-of-annona-muricata-l-fruit-pulp
#12
Natacha Bonneau, Timothé Cynober, Jean-Christophe Jullian, Pierre Champy
INTRODUCTION: Annonaceous acetogenins (AAGs) constitute a group of environmental neurotoxins, possibly implicated in sporadic atypical Parkinsonism/dementia complexes. The recent evidencing of complex mixtures of AAGs in edible fruits and derived food products requires efficient and practical analytical tools for an estimation of human exposure. OBJECTIVE: To develop a simple method for the direct quantitation of the majority of AAGs (sub-types 1a and 1b) within crude extracts, using commonly available (1) H-NMR spectrometers, for food control...
January 16, 2017: Phytochemical Analysis: PCA
https://www.readbyqxmd.com/read/28092417/dense-semi-clathrates-at-high-pressure-a-study-of-the-water-tert-butylamine-system
#13
Rubén Granero-García, Andrzej Falenty, Francesca Paola Anna Fabbiani
In situ high-pressure crystallization and diffraction techniques have been applied to obtain two very structurally-distinct semi-clathrates of the tert-butylamine-water system with hydration numbers 5.65 and 5.8, respectively, thereby considerably reducing a notable hydration gap between the monohydrate and the 7¼-hydrate that results when crystallization space is explored by temperature alone. Both structures can be considered as an intriguing solid-state example of hydrophobic hydration in which the water network creates wide tert-butylamine-filled channels stabilized by cross-linking hydrogen bonds...
January 16, 2017: Chemistry: a European Journal
https://www.readbyqxmd.com/read/28092404/metformin-versus-myoinositol-which-is-better-in-obese-pcos-patients-a-randomized-controlled-crossover-study
#14
Valeria Tagliaferri, Daniela Romualdi, Valentina Immediata, Simona De Cicco, Christian Di Florio, Antonio Lanzone, Maurizio Guido
CONTEXT: due to the central role of metabolic abnormalities in the pathophysiology of PCOS, insulin sensitising agents have been proposed as a feasible treatment option. OBJECTIVE: to investigate which is the more effective between metformin and myoinositol on hormonal, clinical and metabolic parameters in obese patients with polycystic ovary syndrome (PCOS). STUDY DESIGN: crossover randomized-controlled study. PATIENTS: Thirty-four PCOS obese women (age: 25...
January 16, 2017: Clinical Endocrinology
https://www.readbyqxmd.com/read/28092384/emerging-investigator-series-a-14-year-depositional-ice-record-of-perfluoroalkyl-substances-in-the-high-arctic
#15
John J MacInnis, Katherine French, Derek C G Muir, Christine Spencer, Alison Criscitiello, Amila O De Silva, Cora J Young
To improve understanding of long-range transport of perfluoroalkyl substances to the High Arctic, samples were collected from a snow pit on the Devon Ice Cap in spring 2008. Snow was analyzed for perfluoroalkyl acids (PFAAs), including perfluoroalkyl carboxylic acids (PFCAs) and perfluoroalkyl sulfonic acids (PFSAs), as well as perfluorooctane sulfonamide (FOSA). PFAAs were detected in all samples dated from 1993 to 2007. PFAA fluxes ranged from <1 to hundreds of ng per m(2) per year. Flux ratios of even-odd PFCA homologues were mostly between 0...
January 16, 2017: Environmental Science. Processes & Impacts
https://www.readbyqxmd.com/read/28092382/a-vascularized-and-perfused-organ-on-a-chip-platform-for-large-scale-drug-screening-applications
#16
Duc T T Phan, Xiaolin Wang, Brianna M Craver, Agua Sobrino, Da Zhao, Jerry C Chen, Lilian Y N Lee, Steven C George, Abraham P Lee, Christopher C W Hughes
There is a growing awareness that complex 3-dimensional (3D) organs are not well represented by monolayers of a single cell type - the standard format for many drug screens. To address this deficiency, and with the goal of improving screens so that drugs with good efficacy and low toxicity can be identified, microphysiological systems (MPS) are being developed that better capture the complexity of in vivo physiology. We have previously described an organ-on-a-chip platform that incorporates perfused microvessels, such that survival of the surrounding tissue is entirely dependent on delivery of nutrients through the vessels...
January 16, 2017: Lab on a Chip
https://www.readbyqxmd.com/read/28092361/designed-cell-consortia-as-fragrance-programmable-analog-to-digital-converters
#17
Marius Müller, Simon Ausländer, Andrea Spinnler, David Ausländer, Julian Sikorski, Marc Folcher, Martin Fussenegger
Synthetic biology advances the rational engineering of mammalian cells to achieve cell-based therapy goals. Synthetic gene networks have nearly reached the complexity of digital electronic circuits and enable single cells to perform programmable arithmetic calculations or to provide dynamic remote control of transgenes through electromagnetic waves. We designed a synthetic multilayered gaseous-fragrance-programmable analog-to-digital converter (ADC) allowing for remote control of digital gene expression with 2-bit AND-, OR- and NOR-gate logic in synchronized cell consortia...
January 16, 2017: Nature Chemical Biology
https://www.readbyqxmd.com/read/28092166/subchronic-metformin-pretreatment-enhances-novel-object-recognition-memory-task-in-forebrain-ischemia-behavioural-molecular-and-electrophysiological-studies
#18
Ghorbangol Ashabi, Alireza Sarkaki, Fariba Khodagholi, Shima Zareh Shahamati, Mahdi Goudarzvand, Yaghoob Farbood, Mohammad Badavi, Leila Khalaj
Metformin exerts its effect via AMP-activated protein kinase (AMPK), which is a key sensor for energy homeostasis that regulates different intracellular pathways. Metformin attenuates oxidative stress and cognitive impairment. In our experiment, rats were divided into 8 groups; some were pretreated with metformin (Met, 200 mg/kg) and (or) the AMPK inhibitor Compound C (CC) for 14 days. On day 14, rats underwent transient forebrain global ischemia. Data indicated that pretreatment of ischemic rats with metformin reduced working memory deficits in a novel object recognition test compared to group with ischemia-reperfusion (I-R) (P < 0...
November 4, 2016: Canadian Journal of Physiology and Pharmacology
https://www.readbyqxmd.com/read/28092155/discovery-of-first-in-class-potent-and-orally-bioavailable-eed-inhibitor-with-robust-anti-cancer-efficacy
#19
Ying Huang, Jeff Zhang, Zhengtian Yu, Hailong Zhang, Youzhen Wang, Andreas Lingel, Wei Qi, X Justin Gu, Kehao Zhao, Michael David Shultz, Long Wang, Xingnian Fu, Yongfeng Sun, Qiong Zhang, Xiangqing Jiang, Jiang-Wei Zhang, Chunye Zhang, Ling Li, Jue Zeng, Lijian Feng, Chao Zhang, Yueqin Liu, Man Zhang, Lijun Zhang, Mengxi Zhao, Zhenting Gao, Xianghui Liu, Douglas Fang, Haibing Guo, Yuan Mi, Tobias Gabriel, Michael P Dillon, Peter Atadja, Counde Oyang
Overexpression and somatic heterozygous mutations of EZH2, the catalytic subunit Polycomb repressive complex 2 (PRC2), are associated with several tumor types. EZH2 inhibitor, EPZ-6438 (Tazemetostat), demonstrated clinical efficacy in patients with acceptable safety profile as monotherapy. EED, another subunit of PRC2 complex, is essential for its histone methyltransferase activity through direct binding to trimethylated lysine 27 on histone 3 (H3K27Me3). Herein we disclose the discovery of a first-in-class potent, selective and orally bioavailable EED inhibitor EED226 (compound 43)...
January 16, 2017: Journal of Medicinal Chemistry
https://www.readbyqxmd.com/read/28092137/isolation-and-characterization-of-rhizobium-sp-strain-ys-1r-that-degrades-lignin-in-plant-biomass
#20
Colin A Jackson, Matthew B Couger, Madhu Prabhakaran, Karthikeyan D Ramachandriya, Patricia Canaan, Babu Z Fathepure
AIMS: The aim of this work was to isolate novel lignin degrading organisms. METHODS AND RESULTS: Several pure cultures of bacteria that degrade lignin were isolated from bacterial consortia developed from decaying biomass. Among the isolates, Rhizobium sp. strain YS-1r (closest relative of Rhizobium petrolearium Strain SL-1) was explored for its lignin degrading ability. Microcosm studies showed that strain YS-1r was able to degrade a variety of lignin monomers, dimers, and also native lignin in switchgrass and alfalfa...
January 16, 2017: Journal of Applied Microbiology
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