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Wei Du, Qiangshuai Gu, Yang Li, Zhenyang Lin, Dan Yang
The catalyst system of Pd(TFA)2/(S,S)-diPh-pyrox is reported to promote the highly efficient enantioselective oxidative cascade cyclization of alkene-tethered aliphatic acrylamides under mild aerobic conditions. A series of pyrrolizidine derivatives have been synthesized in good yield and excellent enantioselectivity. Deuterium-labeling experiments have revealed that the reaction proceeded through an anti-aminopalladation (anti-AP) pathway with high selectivity. The transition states for the anti-AP step have been calculated to account for the observed enantioselectivity...
January 9, 2017: Organic Letters
Bilal Iqbal Avan, Della Berhanu, Nasir Umar, Deepthi Wickremasinghe, Joanna Schellenberg
Low-resource settings often have limited use of local data for health system planning and decision-making. To promote local data use for decision-making and priority setting, we propose an adapted framework: a data-informed platform for health (DIPH) aimed at guiding coordination, bringing together key data from the public and private sectors on inputs and processes. In working to transform this framework from a concept to a health systems initiative, we undertook a series of implementation research activities including background assessment, testing and scaling up of the intervention...
September 2016: Health Policy and Planning
Qian Sun, Ruifeng Mao, Dongling Wang, Changyan Hu, Yang Zheng, Dequn Sun
Praziquantel (PZQ) is prescribed as a racemic mixture (racemic-PZQ, rac-PZQ), which is composed of (R)-PZQ and (S)-PZQ. In this work, the cytotoxicity of rac-PZQ and its two enantiomers (R)-PZQ and (S)-PZQ on eight cell lines (L-02, HepG2, prf-plc-5, SH-SY5Y, HUVEC, A549, HCT-15, Raw264.7) was evaluated by 3-(4,5-dimethylthiazol-2-yl)-2,5-diphe-nyltetrazolium bromide and lactate dehydrogenase assays. The morphology of apoptotic cells was studied by fluorescence microscope using Hoechst 33342 staining, and the cytotoxicity of the compounds was also tested by lactate dehydrogenase assay...
2016: Drug Design, Development and Therapy
Arun Suneja, Vishnumaya Bisai, Vinod K Singh
A unified approach for the asymmetric syntheses of medicinally important isoindolinones (S)-PD 172938 and (R)-JM 1232 has been accomplished via a Cu(I)-PYBOX-diPh catalyzed highly enantioselective (up to 99% ee) alkynylation/lactamization sequence in a one-pot fashion. The overall sequence involves one C-C and two C-N bond forming events in one pot starting from inexpensive starting material in ambient reaction conditions.
June 3, 2016: Journal of Organic Chemistry
A N Severyukhina, N V Petrova, K Smuda, G S Terentyuk, B N Klebtsov, R Georgieva, H Bäumler, D A Gorin
Novel chitosan-based nanofibrous composite materials containing different amounts of the photosensitizer Photosens were obtained by electrospinning and were characterized by scanning electron microscopy and by confocal laser scanning microscopy. The release of Photosens from the materials was investigated in water and in phosphate-buffered saline. A noncancerous (MC3T3-E1 murine osteoblasts) and a cancerous [T-47D (mammary gland)] cell line were cultivated on Photosens-containing scaffolds, and cell growth and metabolic activity were examined by confocal laser scanning microscopy and by 3-(4,5-dimethylthiazol-2-yl)-2,5-diphe-nyltetrazolium bromide assay, respectively...
August 1, 2016: Colloids and Surfaces. B, Biointerfaces
Aymeric Rouchaud, Waleed Brinjikji, Giuseppe Lanzino, Harry J Cloft, Ramanathan Kadirvel, David F Kallmes
INTRODUCTION: Delayed aneurysm rupture and delayed intraparenchymal hemorrhages (DIPH) are poorly understood and often fatal complications of flow diversion (FD) for intracranial aneurysms. The purpose of this study was to identify risk factors for these complications. METHODS: We performed a systematic review on post-FD delayed aneurysm rupture and DIPH. For each reported case, we collected the following information: aneurysm location, size and rupture status, type of flow diverter used, timing of the hemorrhage, and neurological outcome...
February 2016: Neuroradiology
Vishnumaya Bisai, Arun Suneja, Vinod K Singh
An unprecedented Cu(I)-pybox-diPh-catalyzed highly enantioselective (up to >99% ee) alkynylation/lactamization cascade has been developed as a general catalytic system for the synthesis of diversely substituted isoindolinones of immense biological importance. The cascade effects one C-C and two C-N bond-forming events in one reaction vessel under operationally simple, additive-free reaction conditions in good to excellent yields. The methodology was further extended to the synthesis of tetrahydroisoquinoline scaffolds common to several biologically active natural products in a two-step sequence with remarkable selectivity (up to 94% ee)...
September 26, 2014: Angewandte Chemie
Liu Ying, Zhu Zu-An, Liu Qing-Hua, Kong Qing-Yan, Liu Lei, Cui Tao, Wu Yong-Ping
To investigate the role of RAD001 in the reversing of drug resistance of SGC7901/DDP, we cultured SGC7901/DDP cells with different groups of drugs (RAD001, cisplatin (DDP) alone, or the combination of RAD001 and DDP); after that, we detected the drug sensitivity, cell apoptosis, and levels of P-gp, MRP1, and survivin in the cells of SGC7901/DDP by MTT (3-(4, 5-dimethylthiazol-2-yl)-2, 5-diphe-nyltetrazolium bromide) assay, flow cytometry, immunohistochemical analysis, and Western blot analysis. There was no significant difference between DDP 2...
September 2014: Tumour Biology: the Journal of the International Society for Oncodevelopmental Biology and Medicine
Joo Hyun Lee, Han-Beom Lee, Gum O Jung, Jung Taek Oh, Dong Eun Park, Kwon Mook Chae
PURPOSE: To investigate the chemotherapeutic effect of quercetin against cancer cells, signaling pathway of apoptosis was explored in human pancreatic cells. METHODS: Various anticancer drugs including adriamycin, cisplatin, 5-fluorouracil (5-FU) and gemcitabine were used. Cell viability was measured by 3-[4,5-dimethylthiazol-2-yl]-2,5-diphe-nyltetra zolium bromide assay. Apoptosis was determined by 4'-6-diamidino-2-phenylindole nuclei staining and flow cytometry in PANC-1 cells treated with 50 µg/mL quercetin for 24 hours...
December 2013: Journal of the Korean Surgical Society
Wenhao Weng, Qiong Wu, Yongchun Yu, Wenjie Mei, Xinghe Wang
AIM: Organometallic arene Ru(II) complexes have long been considered as most promising substitutes for cisplatinum as an anti-tumor drug, with low toxicity towards human normal cells and high selectivity to tumor cells. In this study, we synthesized a novel arene Ru(II) drug named Rawq01. We evaluated its activity in an in vitro model of esophageal cancer (ESCC) and further explored the cellular signaling pathways altered by Rawq01. MATERIALS AND METHODS: 3-(4,5-Dimethylthiazol-2-yl)-2,5-diphe nyltetrazolium bromide (MTT) assay, colony forming assay and apoptosis assays were used to evaluate the antitumor activity of Rawq01...
December 2013: Anticancer Research
Catherine Tomas, Azzedine Benaissa, Denis Herbreteau, Krzysztof Kadziolka, Laurent Pierot
INTRODUCTION: The use of flow diverters (FDs) has shown promising results, particularly in the treatment of large or complex intracranial aneurysms. However, some complications can occur both during and after FD treatment, including delayed ipsilateral parenchymal hemorrhage (DIPH). The clinical presentation, etiopathogeny, and management of this complication are not well understood. We report a series of four patients with DIPH and discuss the potential mechanisms and modalities of treatment...
February 2014: Neuroradiology
Jie Zhang, Nannan Tong, Youran Chen, Peichun Li, Sen Yang, Xiaoyan Zhao
Vinorebine (VNR), a second-generation vinca alkaloid antitumor drug, caused serious local venous toxicities, such as venous irritation, phlebitis and necrotizing vasculitis. This study investigated whether resveratrol (RES), a naturally occurring polyphenol compound, could reduce the vascular injury induced by VNR. Human vascular endothelial cell line ECV-304 cells were exposed to VNR for 10 min and then cells were cultured with serum-free medium with or without RES for 24 h. MTT (3-[4, 5-dimethyl-2-thiazolyl]-2, 5-diphe-nyl-2-tetrazolium bromide) assay was used to detect the cell viability...
November 2013: Toxicology Mechanisms and Methods
Daqing Gao, Jiangwen Hu, Xiang Zhang, Chong Gao, Jie Hong
PURPOSE: Human 8-oxoguanine DNA glycosylase (hOGG1) is an ubiquitous protein. It initiates the DNA base excision repair (BER) pathway to repair the 8-oxoguanine lesion. This may be associated with chemotherapeutics. In this article, the effect of hOGG1 over-expression on cisplatin resistance in esophageal squamous cell carcinoma (ESCC) EC9706 and ET13 cells was investigated. METHODS: Recombinant adenovirus pAd/CMV/V5-DEST-hogg1 and control adenovirus pAd/CMV/5-GW/lacZ were constructed and transferred into EC9706 and ET13 cells, respectively...
July 2013: Cancer Biotherapy & Radiopharmaceuticals
Subhrajit Rout, Sumit K Ray, Vinod K Singh
A chiral PYBOX-DIPH-Zn(II) catalyzed enantioselective Mukaiyama-Michael reaction of acyclic silyl enol ethers with 2-enoylpyridine N-oxides has been studied in external additive free conditions at ambient temperature. The methodology offers straightforward access to a variety of functionalized chiral 1,5-dicarbonyl compounds, which could easily be elaborated into synthetically viable pyrones via hydrolysis followed by cyclization. A transition state model has been proposed to explain the stereochemical outcome...
July 21, 2013: Organic & Biomolecular Chemistry
Sumit K Ray, Subhrajit Rout, Vinod K Singh
An enantioselective Michael addition of cyclic 1,3-dicarbonyls to 2-enoylpyridine N-oxides catalyzed by a chiral pybox-diph-Zn(II) complex has been developed. The corresponding Michael adducts have been obtained in high yields with up to >99% ee. The Michael adduct has been transformed to biologically active 2,4-disubstituted hexahydroquinoline. A plausible transition-state model has been proposed to explain the stereochemical outcome of the reaction.
April 21, 2013: Organic & Biomolecular Chemistry
Sumit K Ray, Pradeep K Singh, Nagaraju Molleti, Vinod K Singh
A potential pharmacologically active chiral 3-substituted 4-hydroxy-2-oxo-2H-chromene skeleton has been synthesized by enantioselective Michael addition catalyzed by PYBOX-DIPH-Zn(OTf)(2) complex. The methodology has successfully been employed in the synthesis of (R)-Warfarin and another related compounds.
October 5, 2012: Journal of Organic Chemistry
Guido J Reiss, Michaela K Meyer
The title molecular salt, C(6)H(16)N(+)·CH(3)SO(3) (-), has been determined at 150 K. Two diisopropyl-ammonium cations (dipH) and two anions form N-H⋯O hydrogen-bonded cyclic dimers lying around centers of symmetry. Only two of the three O atoms of the methane-sulfonate anion are involved in hydrogen bonding, resulting in slightly longer S-O bond lengths. The title structure represents an example of a sulfonate anion that is part of a hydrogen-bonding R(4) (4)(12) graph-set motif, which is well known for related dipH acetates...
August 1, 2011: Acta Crystallographica. Section E, Structure Reports Online
Kathryn Hinsliff-Smith, Peter Gates, Marion Leducq
In 2006, the United Kingdom (U.K.) Department of Health (DoH) produced guidelines, requiring institutions to address the attrition rates for student nurses and midwives. This issue is not only a concern in the U.K. but has gained prominence in other Schools of Nursing including the U.S.A., Australia, and developing countries. Many Schools of Nursing have witnessed a change in their student population with a growing prominence of mature entrants (those over 21). Studies that focus on learner persistence, in particular mature students are relatively rare and very scarce on entrants with an Access to Higher Education (HE) qualification...
January 2012: Nurse Education Today
Jayne H Donaldson, Jacqueline McCallum, Patricia Lafferty
AIM: To gain an understanding of patterns of retention and attrition for student nurses on the diploma of higher education (DipHE)/bachelor of science (B.Sc.) (adult) on completion of the common foundation programme (CFP=year 1 of the programme). METHOD: A questionnaire called the "interview score sheet" (ISS) collected data on six cohorts from a Higher Education Institution in Scotland. At the initial recruitment interview each candidate was scored independently by two interviewers on the ISS...
October 2010: Nurse Education Today
Pradeep K Singh, Vinod K Singh
A highly enantioselective Friedel-Crafts alkylation of pyrroles with 2-enoylpyridine N-oxides catalyzed by chiral PYBOX-DIPH-Zn(II) complexes has been developed. The catalyst offers substantial substrate scope and furnished alkylated pyrroles in excellent yields (up to 99%) and enantioselectivities (up to >99% ee).
January 1, 2010: Organic Letters
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