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https://www.readbyqxmd.com/read/28177239/visible-light-copper-photoredox-catalyzed-aerobic-oxidative-cou-pling-of-phenol-and-terminal-alkynes-regioselctive-synthesis-of-functionalized-ketones-via-c%C3%AF-%C2%BAc-triple-bond-cleavage
#1
Arunachalam Sagadevan, Vaibhav Pramod Charpe, Ayyakkannu Ragupathi, Kuo-Chu Hwang
Direct oxidative coupling of phenols and terminal alkynes were achieved at room temperature by visible light-mediated copper-catalyzed process. This method allows for regioselective synthesis of hydroxyl-functionalized aryl and alkyl ketones from simple phenols and phenylacetylene via CC triple bond cleavage. 47 examples were presented. From synthetic point view, this protocol offers an efficient synthetic route for preparation of pharmaceutical drugs, such as, pitofenone and fenofibrate.
February 8, 2017: Journal of the American Chemical Society
https://www.readbyqxmd.com/read/28170238/dual-site-fluorescent-probe-for-visualizing-the-metabolism-of-cys-in-living-cells
#2
Yongkang Yue, Fangjun Huo, Peng Ning, Yongbin Zhang, Jianbin Chao, Xiangming Meng, Caixia Yin
Fluorescent probes as non-invasive tools to visualize the metabo-lism of bio-molecules hold great potential to explore their physio-logical and pathological processes. For cysteine (Cys), however, none of the reported fluorescent probes could image the metabolic processes in living cells. To achieve this goal, we developed a cou-marin derivate based on the rational design of the dual recognition sites for Cys and its metabolite SO2, respectively. The probe displayed distinct two channels turn-on fluorescent emission towards Cys and SO2, which were successfully applied for both A549 cells and zebra fish imaging...
February 7, 2017: Journal of the American Chemical Society
https://www.readbyqxmd.com/read/28133669/remarkable-influence-of-phane-effect-on-the-excited-state-properties-of-cofacially-oriented-coumarins
#3
Arindam Mukhopadhyay, Vijay Kumar Maka, Jarugu Narasimha Moorthy
A comprehensive investigation of the photophysics of a cofacially oriented bis-coumarin based on naphthalene, i.e., Cou-Nap, designed and synthesized to examine the influence of π-electronic communication between the two fluorophores, reveals exceptional excited-state properties. While the anticipated [2 + 2] photocycloaddition is not observed despite the fact that the two reactive coumarin units are at a distance of 3.8 Å, the fluorescence quantum yields and singlet lifetimes in different solvents are found to be remarkably higher when compared to those of the parent coumarin and a mono-coumarin model system, i...
January 30, 2017: Physical Chemistry Chemical Physics: PCCP
https://www.readbyqxmd.com/read/28068060/structural-and-functional-basis-of-c-methylation-of-coumarin-scaffolds-by-novo
#4
Joanna C Sadler, Chun-Wa H Chung, Julie E Mosley, Glenn A Burley, Luke D Humphreys
C-methylation of aromatic small molecules by C-methyltransferases (C-MTs) is an important biological transformation that involves C-C bond formation using S-adenosyl-l-methionine (SAM) as the methyl donor. Here, two advances in the mechanistic understanding of C-methylation of the 8-position of coumarin substrates catalyzed by the C-MT NovO from Streptomyces spheroides are described. First, a crystal structure of NovO reveals the Arg116-Asn117 and His120-Arg121 motifs are essential for coumarin substrate binding...
January 13, 2017: ACS Chemical Biology
https://www.readbyqxmd.com/read/28065602/diagnostic-and-therapeutic-strategy-in-meni%C3%A3-re-s-disease-guidelines-of-the-french-otorhinolaryngology-head-and-neck-surgery-society-sforl
#5
J Nevoux, V Franco-Vidal, D Bouccara, C Parietti-Winkler, A Uziel, A Chays, X Dubernard, V Couloigner, V Darrouzet, T Mom
OBJECTIVES: The authors present the guidelines of the French Otorhinolaryngology-Head and Neck Surgery Society (Société française d'oto-rhino-laryngologie et de chirurgie de la face et du cou: SFORL) for diagnostic and therapeutic strategy in Menière's disease. METHODS: A work group was entrusted with a review of the scientific literature on the above topic. Guidelines were drawn up, then read over by an editorial group independent of the work group. The guidelines were graded according to the literature analysis and recommendations grading guide published by the French National Agency for Accreditation and Evaluation in Health (January 2000)...
January 3, 2017: European Annals of Otorhinolaryngology, Head and Neck Diseases
https://www.readbyqxmd.com/read/28058432/hydroxyl-radical-production-induced-by-plasma-hydrogenated-nanodiamonds-under-x-ray-irradiation
#6
Magdalena Kurzyp, Hugues A Girard, Yannis Cheref, Emilie Brun, Cecile Sicard-Roselli, Samuel Saada, Jean-Charles Arnault
For the first time, overproduction of hydroxyl radicals (HO˙) induced by plasma hydrogenated detonation nanodiamonds (H-NDs) under X-ray irradiation is reported. Using coumarin (COU) as a fluorescent probe, we reveal a significant increase of 40% of the HO˙ production in the presence of H-NDs (6-100 μg ml(-1)) compared with water alone. This effect is related to the negative electron affinity of the hydrogenated nanodiamonds and illustrates the ability of H-NDs to produce reactive oxygen species probably via electron emission in water under X-ray irradiation...
January 19, 2017: Chemical Communications: Chem Comm
https://www.readbyqxmd.com/read/27986467/guidelines-of-the-french-society-of-otorhinolaryngology-sforl-short-version-specific-treatment-of-epistaxis-in-rendu-osler-weber-disease
#7
L Robard, J Michel, V Prulière Escabasse, E Bequignon, B Vérillaud, O Malard, L Crampette
OBJECTIVES: The authors present the guidelines of the French Oto-Rhino-Laryngology - Head and Neck Surgery Society (Société Française d'Oto-Rhino-Laryngologie et de Chirurgie de la Face et du Cou: SFORL) concerning specific treatment of epistaxis in Rendu-Osler-Weber disease. METHODS: A multidisciplinary work-group was entrusted with a review of the scientific literature on the above topic. Guidelines were drawn up, based on the articles retrieved and the group members' individual experience...
December 13, 2016: European Annals of Otorhinolaryngology, Head and Neck Diseases
https://www.readbyqxmd.com/read/27858544/current-role-of-surgery-in-the-management-of-oropharyngeal-cancer
#8
Meghan T Turner, J Kenneth Byrd, Robert L Ferris
The 1990s saw an increased use of chemoradiotherapy protocols, commonly referred to as organ-sparing therapy, for the treatment of oropharyngeal cancer after the Groupe d'Oncologie Radiothérapie Tête et Cou trial. Since that time, human papillomavirus-associated oropharyngeal squamous cell carcinoma has been identified as a unique disease, with improved survival regardless of treatment modality. The improved outcomes of this population has led to re-evaluation of treatment paradigms in the past decade, with a desire to spare young, human papillomavirus-positive patients the treatment-related toxicities of chemoradiotherapy and to use new minimally invasive surgical techniques to improve outcomes...
November 2016: Journal of Oncology Practice
https://www.readbyqxmd.com/read/27774655/phenolic-compounds-alone-or-in-combination-may-be-involved-in-propolis-effects-on-human-monocytes
#9
Eliza de Oliveira Cardoso, Bruno José Conti, Karina Basso Santiago, Fernanda Lopes Conte, Lucas Pires Garcia Oliveira, Rodrigo Tavanelli Hernandes, Marjorie de Assis Golim, José Maurício Sforcin
OBJECTIVES: Propolis is a natural product with a complex chemical composition. Its isolated compounds exert biological activities; however, its synergistic effects are unknown. The involvement of phenolic acids (caffeic - Caf, dihydrocinnamic - Cin and p-coumaric - Cou) alone or in combination was investigated in the action of propolis in human monocytes. METHODS: Cell viability was analysed by MTT assay; TNF-α, IL-6 and IL-10 production by enzyme-linked immunosorbent assay (ELISA); cell markers expression by flow cytometry; colony-forming units were counted to assess the microbicidal activity; and H2 O2 production was analysed by colorimetric assay...
January 2017: Journal of Pharmacy and Pharmacology
https://www.readbyqxmd.com/read/27765622/guidelines-of-the-french-society-of-otorhinolaryngology-sforl-second-line-treatment-of-epistaxis-in-adults
#10
B Verillaud, L Robard, J Michel, V Pruliere Escabasse, E Béquignon, L Crampette, O Malard
OBJECTIVES: The authors present the guidelines of the French Oto-Rhino-Laryngology - Head and Neck Surgery Society (Société Française d'Oto-Rhino-Laryngologie et de Chirurgie de la Face et du Cou: SFORL) on second-line treatment of epistaxis in adults, after failure of anterior and/or anterior-posterior nasal packing. METHODS: A multidisciplinary work group was entrusted with a review of the scientific literature on the above topic. Guidelines were drawn up, based on the articles retrieved and the group members' individual experience...
October 17, 2016: European Annals of Otorhinolaryngology, Head and Neck Diseases
https://www.readbyqxmd.com/read/27763536/fluid-biomarkers-of-traumatic-brain-injury-and-intended-context-of-use
#11
REVIEW
Tanya Bogoslovsky, Jessica Gill, Andreas Jeromin, Cora Davis, Ramon Diaz-Arrastia
Traumatic brain injury (TBI) is one of the leading causes of death and disability around the world. The lack of validated biomarkers for TBI is a major impediment to developing effective therapies and improving clinical practice, as well as stimulating much work in this area. In this review, we focus on different settings of TBI management where blood or cerebrospinal fluid (CSF) biomarkers could be utilized for predicting clinically-relevant consequences and guiding management decisions. Requirements that the biomarker must fulfill differ based on the intended context of use (CoU)...
October 18, 2016: Diagnostics
https://www.readbyqxmd.com/read/27726975/guidelines-of-the-french-society-of-otorhinolaryngology-sforl-epistaxis-and-high-blood-pressure
#12
J Michel, V Prulière Escabasse, E Bequignon, B Vérillaud, L Robard, L Crampette, O Malard
OBJECTIVES: The authors present the guidelines of the French Oto-Rhino-Laryngology - Head and Neck Surgery Society (Société Française d'Oto-Rhino-Laryngologie et de Chirurgie de la Face et du Cou: SFORL) on epistaxis in high blood pressure. METHODS: A multidisciplinary work group was entrusted with a review of the scientific literature on the above topic. Guidelines were drawn up, based on the articles retrieved and the group members' individual experience. They were then read over by an editorial group independent of the work group...
October 7, 2016: European Annals of Otorhinolaryngology, Head and Neck Diseases
https://www.readbyqxmd.com/read/27723324/plasmonically-engineered-nanoprobes-for-biomedical-applications
#13
Amit Kumar, Sungi Kim, Jwa-Min Nam
The localized surface plasmon resonance of metal nanoparticles is the collective oscillation of electrons on particle surface, induced by incident light, and is a particle composition-, morphology-, and coupling-dependent property. Plasmonic engineering deals with highly precise formation of the targeted nanostructures with targeted plasmonic properties (e.g., electromagnetic field distribution and enhancement) via controlled synthetic, assembling, and atomic/molecular tuning strategies. These plasmonically engineered nanoprobes (PENs) have a variety of unique and beneficial physical, chemical, and biological properties, including optical signal enhancement, catalytic, and local temperature-tuning photothermal properties...
November 9, 2016: Journal of the American Chemical Society
https://www.readbyqxmd.com/read/27685176/ynamides-as-racemization-free-coupling-reagents-for-amide-and-peptide-synthesis
#14
Long Hu, Silin Xu, Zhenguang Zhao, Yang Yang, Zhiyuan Peng, Ming Yang, Changliu Wang, Junfeng Zhao
A highly efficient, two-step, one-pot synthetic strategy for amides and peptides was developed by employing ynamides as novel coupling reagents under extremely mild reaction conditions. The ynamides not only are effective for simple amide and dipeptide synthesis but can also be used for peptide segment condensation. Importantly, no racemization was detected during the activation of chiral carboxylic acids. Excellent amidation selectivity toward amino groups in the presence of -OH, -SH, -CONH2, ArNH2, and the NH of indole was observed, making the protection of these functional groups unnecessary in amide and peptide synthesis...
October 4, 2016: Journal of the American Chemical Society
https://www.readbyqxmd.com/read/27678453/the-added-value-of-circulating-tumour-cell-enumeration-to-standard-markers-in-assessing-prognosis-in-a-metastatic-castration-resistant-prostate-cancer-population
#15
Glenn Heller, Karim Fizazi, Robert T McCormack, Arturo Molina, David MacLean, Iain J Webb, Fred Saad, Johann S de Bono, Howard I Scher
PURPOSE: Metastatic castration-resistant prostate cancer (mCRPC) is a heterogeneous disease for which better prognostic models for survival are needed. We examined the added value of circulating tumor cell (CTC) enumeration relative to common prognostic laboratory measures from CRPC patients. Experimental Technique: Utility of CTC enumeration as a baseline and postbaseline prognostic biomarker was examined using data from two prospective randomized registration-directed trials (COU-AA-301 and ELM-PC4) within statistical models used to estimate risk for survival...
September 27, 2016: Clinical Cancer Research: An Official Journal of the American Association for Cancer Research
https://www.readbyqxmd.com/read/27670718/impact-of-single-agent-daily-prednisone-on-outcomes-in-men-with-metastatic-castration-resistant-prostate-cancer
#16
G Sonpavde, G R Pond, A J Templeton, E D Kwon, J S De Bono
BACKGROUND: Despite palliative benefits and PSA responses, the objective clinical impact of daily oral prednisone (P) for metastatic castration-resistant prostate cancer (mCRPC) is unknown. We performed a pooled analysis of control arms of randomized trials that either did or did not administer single-agent P to evaluate its impact on overall survival (OS) and toxicities. METHODS: Individual patient data from control arms of randomized trials of men with mCRPC who received placebo or P+placebo post docetaxel were eligible for analysis...
September 27, 2016: Prostate Cancer and Prostatic Diseases
https://www.readbyqxmd.com/read/27570999/number-needed-to-treat-and-associated-incremental-costs-of-treatment-with-enzalutamide-versus-abiraterone-acetate-plus-prednisone-in-chemotherapy-na%C3%A3-ve-patients-with-metastatic-castration-resistant-prostate-cancer
#17
Marjan Massoudi, Mark Balk, Hongbo Yang, Cat N Bui, Bhavik J Pandya, Jenny Guo, Yan Song, Eric Q Wu, Bruce Brown, Arie Barlev, Scott Flanders
OBJECTIVE: Enzalutamide (ENZA) and abiraterone acetate plus prednisone (AA) are approved second-generation hormone therapies for chemotherapy-naïve metastatic castration-resistant prostate cancer (mCRPC). This study compared ENZA with AA in chemotherapy-naïve mCRPC by calculating the number needed to treat (NNT) and associated incremental costs to achieve one additional chemotherapy-naïve patient with mCRPC free of radiographic progression, chemotherapy, or death over a 1-year time horizon...
February 2017: Journal of Medical Economics
https://www.readbyqxmd.com/read/27566699/abiraterone-acetate-for-the-treatment-of-chemotherapy-na%C3%A3-ve-metastatic-castration-resistant-prostate-cancer-an-evidence-review-group-perspective-of-an-nice-single-technology-appraisal
#18
REVIEW
Bram L T Ramaekers, Rob Riemsma, Florian Tomini, Thea van Asselt, Sohan Deshpande, Steven Duffy, Nigel Armstrong, Johan L Severens, Jos Kleijnen, Manuela A Joore
The National Institute for Health and Care Excellence (NICE) invited Janssen, the company manufacturing abiraterone acetate (AA; tradename Zytiga(®)), to submit evidence for the clinical and cost effectiveness of AA in combination with prednisone/prednisolone (AAP) compared with watchful waiting (i.e. best supportive care [BSC]) for chemotherapy-naïve patients with metastatic castration-resistant prostate cancer (mCRPC). Kleijnen Systematic Reviews Ltd (KSR), in collaboration with Maastricht University Medical Center, was commissioned as the Evidence Review Group (ERG)...
February 2017: PharmacoEconomics
https://www.readbyqxmd.com/read/27558921/a-highly-selective-potassium-sensor-for-the-detection-of-potassium-in-living-tissues
#19
Alexis Depauw, Elena Dossi, Naresh Kumar, Céline Fiorini-Debuisschert, Gilles Huberfeld, Minh-Huong Ha-Thi, Nathalie Rouach, Isabelle Leray
The development of highly selective sensors for potassium is of great interest in biology. Two new hydrosoluble potassium sensors (Calix-COU-Alkyne and Calix-COU-Am) based on a calix[4]arene bis(crown-6) and an extended coumarin were synthesized and characterized. The photophysical properties and complexation studies of these compounds have been investigated and show high molar extinction coefficients and high fluorescence quantum yields. Upon complexation with potassium in the millimolar concentration range, an increase of one- and two-photon fluorescence emission is detected...
October 10, 2016: Chemistry: a European Journal
https://www.readbyqxmd.com/read/27544566/how-i-do-it-prescribing-abiraterone-acetate-for-metastatic-castration-resistant-prostate-cancer
#20
Yuding Wang, Shawn Dason, Bobby Shayegan
Abiraterone acetate (AA) is a selective irreversible inhibitor of CYP 17, a key enzyme in androgen biosynthesis. The efficacy and safety of AA in improving survival and quality of life in metastatic castration resistant prostate cancer (mCRPC) has been demonstrated in two landmark clinical trials (COU-AA-301 and COU-AA-302). This article will review the rationale, pharmacology, clinical indications and contraindications, administration, and adverse effects of AA administration in mCRPC.
August 2016: Canadian Journal of Urology
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