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https://www.readbyqxmd.com/read/28431453/carboxymethyl-%C3%AE-cyclodextrin-as-chiral-selector-in-capillary-electrophoresis-enantioseparation-of-16-basic-chiral-drugs-and-its-chiral-recognition-mechanism-associated-with-drugs-structural-features
#1
Linlin Fang, Yueying Du, Xiaoyu Hu, Linda Luo, Xin Guo, Xingjie Guo, Jia Yu
Herein we present the enantioseparation of 10 cardiovascular agents and 6 bronchiectasis drugs including propranolol, carteolol, metoprolol, atenolol, pindolol, esmolol, bisoprolol, bevantolol, arotinolol, sotalol, clenbuterol, procaterol, bambuterol, tranterol, salbutamol and terbutaline sulfate using carboxymethyl-β-cyclodextrin (CM-β-CD) as chiral selector. To our knowledge, there is no literature about using CM-β-CD for separating carteolol, esmolol, bisoprolol, bevantolol, arotinolol, procaterol, bambuterol and tranterol...
April 21, 2017: Biomedical Chromatography: BMC
https://www.readbyqxmd.com/read/28431417/the-occurrence-of-single-and-multiple-organ-dysfunction-in-pediatric-electrical-versus-other-thermal-burns
#2
Gabriel Hundeshagen, Paul Wurzer, Abigail A Forbes, Charles D Voigt, Vanessa N Collins, Janos Cambiaso-Daniel, Celeste C Finnerty, David N Herndon, Ludwik K Branski
BACKGROUND: Multiple organ failure (MOF) is a major contributor to morbidity and mortality in burned children. While various complications induced by electrical injuries have been described, the incidence and severity of single organ failure (SOF) and MOF associated with this type of injury are unknown. The study was undertaken to compare the incidence and severity of SOF and MOF as well as other complications between electrically and thermally burned children. PATIENTS AND METHODS: Between 2001 and 2016, 288 pediatric patients with electrical burns (EB; n = 96) or thermal burns (CTR; n = 192) were analyzed in this study...
May 2017: Journal of Trauma and Acute Care Surgery
https://www.readbyqxmd.com/read/28431397/sensitization-of-tamoxifen-resistant-breast-cancer-cells-by-z-ligustilide-through-inhibiting-autophagy-and-accumulating-dna-damages
#3
Hongyi Qi, Zhuyun Jiang, Chengqiang Wang, Yi Yang, Li Li, Hui He, Zanyang Yu
Autophagy plays a pro-survival role in the tamoxifen-resistant breast cancer cells. Herein we found that autophagy was concomitantly induced in tamoxifen-resistant MCF-7 (MCF-7TR5) cells through the dissociation of Bcl-2 from Beclin 1 and subsequent enhancement of interaction among the ATG14-Beclin1-PI3KC3 complex. Moreover, higher level of DNA damage was observed in MCF-7TR5 cells with the decreased BRCA1 and RAD51 level and the increased Ku80 level. Interestingly, Nur77 was selectively degraded by autophagy, which causes the release of Ku80 from the Nur77-Ku80 complex, resulting in the increase of the DNA binding of Ku80 and DNA-PKcs...
April 4, 2017: Oncotarget
https://www.readbyqxmd.com/read/28431385/a-method-for-evaluating-the-pharmaceutical-deconjugation-potential-in-river-water-environments
#4
Takashi Azuma, Mao Ishida, Kanae Hisamatsu, Ayami Yunoki, Kana Otomo, Mari Kunitou, Mai Shimizu, Kaori Hosomaru, Shiori Mikata, Yoshiki Mino
A new enzymatic assay method that uses deconjugation enzymes was developed to evaluate the presence and extent of conjugated pharmaceuticals in the form of glucuronide conjugates or sulphate conjugates in river environments. First, acetaminophen glucuronide (Ace Glu) and acetaminophen sulphate (Ace Sul) were used as model conjugated pharmaceuticals to determine the appropriate combination of deconjugation enzymes and reaction conditions, including temperature, duration and pH. Next, we applied the defined method to 19 pharmaceuticals grouped into nine therapeutic classes that were chosen based on previously detected levels and frequencies in sewage and river water...
April 10, 2017: Chemosphere
https://www.readbyqxmd.com/read/28431360/contrasting-dual-c-cl-isotope-fractionation-offers-potential-to-distinguish-reductive-chloroethene-transformation-from-breakdown-by-permanganate
#5
Eylem Doğan-Subaşı, Martin Elsner, Shiran Qiu, Stefan Cretnik, Siavash Atashgahi, Orfan Shouakar-Stash, Nico Boon, Winnie Dejonghe, Leen Bastiaens
cis-1,2-Dichloroethene (cis-DCE) and trichloroethene (TCE) are persistent, toxic and mobile pollutants in groundwater systems. They are both conducive to reductive dehalogenation and to oxidation by permanganate. In this study, the potential of dual element (C, Cl) compound specific isotope analyses (CSIA) for distinguishing between chemical oxidation and anaerobic reductive dechlorination of cis-DCE and TCE was investigated. Well-controlled cis-DCE degradation batch tests gave similar carbon isotope enrichment factors εC (‰), but starkly contrasting dual element isotope slopes Δδ(13)C/Δδ(37)Cl for permanganate oxidation (εC=-26‰±6‰, Δδ(13)C/Δδ(37)Cl≈-125±47) compared to reductive dechlorination (εC=-18‰±4‰, Δδ(13)C/Δδ(37)Cl≈4...
April 18, 2017: Science of the Total Environment
https://www.readbyqxmd.com/read/28431354/first-example-of-peptides-targeting-the-dimer-interface-of-leishmania-infantum-trypanothione-reductase-with-potent-in%C3%A2-vitro-antileishmanial-activity
#6
Marta Ruiz-Santaquiteria, Pedro A Sánchez-Murcia, Miguel A Toro, Héctor de Lucio, Kilian Jesús Gutiérrez, Sonia de Castro, Filipa A C Carneiro, Federico Gago, Antonio Jiménez-Ruiz, María-José Camarasa, Sonsoles Velázquez
A series of 9-mer and 13-mer amide-bridged cyclic peptides derived from the linear prototype Ac-PKIIQSVGIS-Nle-K-Nle-NH2 (Toro et al. ChemBioChem2013) has been designed and synthesized by introduction of the lactam between amino acid side chains that are separated by one helical turn (i, i+4). All of these compounds were tested in vitro as both dimerization and enzyme inhibitors of Leishmania infantum trypanothione reductase (Li-TryR). Three of the 13-mer cyclic peptide derivatives (3, 4 and 6) inhibited the oxidoreductase activity of Li-TryR in the low micromolar range and they also disrupted enzyme dimerization...
April 13, 2017: European Journal of Medicinal Chemistry
https://www.readbyqxmd.com/read/28431353/discovery-of-potential-anticancer-multi-targeted-ligustrazine-based-cyclohexanone-and-oxime-analogs-overcoming-the-cancer-multidrug-resistance
#7
Gao-Feng Zha, Hua-Li Qin, Bahaa G M Youssif, Muhammad Wahab Amjad, Maria Abdul Ghafoor Raja, Ahmed H Abdelazeem, Syed Nasir Abbas Bukhari
The drug research and development nowadays is focusing on multi-target drugs. In the treatment of cancer, therapies using drugs inhibiting one numerous targets signify a novel viewpoint. In comparison with traditional therapy, multi-targeted drugs directly aim cell subpopulations which are involved in progression of tumor. The current study comprises the synthesis of 34 novel ligustrazine-containing α, β-unsaturated carbonyl-based compounds and oximes. The growth of 5 various cancer cell types was strongly inhibited by ligustrazine-containing oximes as revealed by biological evaluation...
April 14, 2017: European Journal of Medicinal Chemistry
https://www.readbyqxmd.com/read/28431342/discovery-of-tetrahydrocarbazoles-as-dual-perk-and-prb-inhibitors
#8
Mahesh R Kulkarni, Madhav S Mane, Usha Ghosh, Rajiv Sharma, Nitin P Lad, Ankita Srivastava, Asha Kulkarni-Almeida, Prashant S Kharkar, Vijay M Khedkar, Shivaji S Pandit
The extracellular signal-regulated kinase (ERK) is one of the most important molecular targets for cancer that controls diverse cellular processes such as proliferation, survival, differentiation and motility. Similarly, the Rb (retinoblastoma protein) is a tumor suppressor protein and its function is to prevent excessive cell growth by inhibiting cell cycle progression. When the cell is ready to divide, pRb is phosphorylated, becomes inactive and allows cell cycle progression. Herein, we discovered a new series of tetrahydrocarbazoles as dual inhibitors of pERK and pRb phosphorylation...
March 2, 2017: European Journal of Medicinal Chemistry
https://www.readbyqxmd.com/read/28431341/eco-friendly-synthesis-of-novel-cyanopyridine-derivatives-and-their-anticancer-and-pim-1-kinase-inhibitory-activities
#9
Khaled A M Abouzid, Ghada H Al-Ansary, Abeer M El-Naggar
Targeting Pim-1 kinase recently proved to be profitable for conquering cancer proliferation. In the current study, we report the design, synthesis and biological evaluation of two novel series of 2-amino cyanopyridine series (5a-g) and 2-oxocyanopyridine series (6a-g) targeting Pim-1 kinase. All of the newly synthesized compounds were evaluated for their in vitro anticancer activity against a panel of three cell lines, namely, the liver cancer cell line (HepG2), the colon cancer cell line (HCT-116) and the breast cancer cell line (MCF-7)...
April 14, 2017: European Journal of Medicinal Chemistry
https://www.readbyqxmd.com/read/28431339/novel-coumarin-and-quinolinone-based-polycycles-as-cell-division-cycle-25-a-and-c-phosphatases-inhibitors-induce-proliferation-arrest-and-apoptosis-in-cancer-cells
#10
Clemens Zwergel, Brigitte Czepukojc, Emilie Evain-Bana, Zhanjie Xu, Giulia Stazi, Mattia Mori, Alexandros Patsilinakos, Antonello Mai, Bruno Botta, Rino Ragno, Denise Bagrel, Gilbert Kirsch, Peter Meiser, Claus Jacob, Mathias Montenarh, Sergio Valente
Cell division cycle phosphatases CDC25 A, B and C are involved in modulating cell cycle processes and are found overexpressed in a large panel of cancer typology. Here, we describe the development of two novel quinone-polycycle series of CDC25A and C inhibitors on the one hand 1a-k, coumarin-based, and on the other 2a-g, quinolinone-based, which inhibit either enzymes up to a sub-micro molar level and at single-digit micro molar concentrations, respectively. When tested in six different cancer cell lines, compound 2c displayed the highest efficacy to arrest cell viability, showing in almost all cell lines sub-micro molar IC50 values, a profile even better than the reference compound NCS95397...
April 10, 2017: European Journal of Medicinal Chemistry
https://www.readbyqxmd.com/read/28431335/minimization-of-the-amount-of-kryptofix-222-khco3-for-applications-to-microscale-18-f-radiolabeling
#11
Ren Iwata, Claudio Pascali, Kazunori Terasaki, Yoichi Ishikawa, Shozo Furumoto, Kazuhiko Yanai
Conversion of aqueous [(18)F]fluoride to reactive [(18)F]fluoride is an important first step in the radiosynthesis of (18)F-labeled compounds by nucleophilic substitution. A versatile method for the rapid preparation of reactive [(18)F]fluoride by the combined use of an Oasis MAX cartridge and a methanolic solution of the Kryptofix 222-KHCO3 complex (K.222/KHCO3) was developed. The latter amount was optimized with the aim to keep it as low as possible while achieving recovery yields of [(18)F]fluoride comparable to those attained with the commonly used QMA cartridge...
April 13, 2017: Applied Radiation and Isotopes
https://www.readbyqxmd.com/read/28431320/trehalose-supplementation-reduces-hepatic-endoplasmic-reticulum-stress-and-inflammatory-signaling-in-old-mice
#12
Michael J Pagliassotti, Andrea L Estrada, William M Hudson, Yuren Wei, Dong Wang, Douglas R Seals, Melanie L Zigler, Thomas J LaRocca
The accumulation of damaged proteins can perturb cellular homeostasis and provoke aging and cellular damage. Quality control systems, such as the unfolded protein response (UPR), inflammatory signaling and protein degradation, mitigate the residence time of damaged proteins. In the present study, we have examined the UPR and inflammatory signaling in the liver of young (~6 months) and old (~28 months) mice (n=8/group), and the ability of trehalose, a compound linked to increased protein stability and autophagy, to counteract age-induced effects on these systems...
April 6, 2017: Journal of Nutritional Biochemistry
https://www.readbyqxmd.com/read/28431318/assessing-seasonal-variation-of-synthetic-musks-in-beach-sands-from-oporto-coastal-area-a-case-study
#13
Vera Homem, Inês Magalhães, Arminda Alves, Lúcia Santos
Synthetic musk compounds are widely used in the formulation of several cosmetics, personal care and household products. Due to their massive and widespread use, together with some health concerns, they are considered emerging pollutants and have been detected in different environmental compartments. This study focused on the evaluation of the concentration of synthetic musks (five nitro, five polycyclic and one macrocyclic musks) in beach sands, from Oporto coastal area (Portugal), contributing to the enhancement of the knowledge of levels, trends and behaviour of these compounds in this particular matrix...
April 18, 2017: Environmental Pollution
https://www.readbyqxmd.com/read/28431313/raman-spectroscopy-for-the-characterization-of-different-fractions-of-hemp-essential-oil-extracted-at-130%C3%A2-c-using-steam-distillation-method
#14
Muhammad Asif Hanif, Haq Nawaz, Saima Naz, Rubina Mukhtar, Nosheen Rashid, Ijaz Ahmad Bhatti, Muhammad Saleem
In this study, Raman spectroscopy along with Principal Component Analysis (PCA) is used for the characterization of pure essential oil (pure EO) isolated from the leaves of the Hemp (Cannabis sativa L.,) as well as its different fractions obtained by fractional distillation process. Raman spectra of pure Hemp essential oil and its different fractions show characteristic key bands of main volatile terpenes and terpenoids, which significantly differentiate them from each other. These bands provide information about the chemical composition of sample under investigation and hence can be used as Raman spectral markers for the qualitative monitoring of the pure EO and different fractions containing different active compounds...
April 1, 2017: Spectrochimica Acta. Part A, Molecular and Biomolecular Spectroscopy
https://www.readbyqxmd.com/read/28431308/hyperexcitability-of-inferior-colliculus-and-acoustic-startle-reflex-with-age-related-hearing-loss
#15
Binbin Xiong, Ana'am Alkharabsheh, Senthilvelan Manohar, Guang-Di Chen, Ning Yu, Xiaoming Zhao, Richard Salvi, Wei Sun
Chronic tinnitus and hyperacusis often develop with age-related hearing loss presumably due to aberrant neural activity in the central auditory system (CAS) induced by cochlear pathologies. However, the full spectrum of physiological changes that occur in the CAS as a result age-related hearing loss are still poorly understood. To address this issue, neurophysiological measures were obtained from the cochlea and the inferior colliculus (IC) of 2, 6 and 12 month old C57BL/6J mice, a mouse model for early age-related hearing loss...
March 27, 2017: Hearing Research
https://www.readbyqxmd.com/read/28431285/two-benzoyl-coumarin-amide-fluorescence-chemosensors-for-cyanide-anions
#16
Zian Wang, Qianqian Wu, Jiale Li, Shuang Qiu, Duxia Cao, Yongxiao Xu, Zhiqiang Liu, Xueying Yu, Yatong Sun
Two new benzoyl coumarin amide derivatives with ortho hydroxyl benzoyl as terminal group have been synthesized. Their photophysical properties and recognition properties for cyanide anions in acetonitrile have also been examined. The influence of electron donating diethylamino group in coumarin ring and hydroxyl in benzoyl group on recognition properties was explored. The results indicate that the compounds can recognize cyanide anions with obvious absorption and fluorescence spectral change and high sensitivity...
April 13, 2017: Spectrochimica Acta. Part A, Molecular and Biomolecular Spectroscopy
https://www.readbyqxmd.com/read/28431277/endocrine-disruption-by-environmental-gestagens-in-amphibians-a-short-review-supported-by-new-in%C3%A2-vitro-data-using-gonads-of-xenopus-laevis
#17
REVIEW
Andrea Ziková, Claudia Lorenz, Frauke Hoffmann, Wibke Kleiner, Ilka Lutz, Matthias Stöck, Werner Kloas
Endocrine disruption caused by various anthropogenic compounds is of persisting concern, especially for aquatic wildlife, because surface waters are the main sink of these so-called endocrine disruptors (ED). In the past, research focused on (anti)estrogenic, (anti)androgenic, and (anti)thyroidal substances, affecting primarily reproduction and development in vertebrates; however, other endocrine systems might be also targeted by ED. Environmental gestagens, including natural progestogens (e.g. progesterone (P4)) and synthetic progestins used for contraception, are supposed to affect vertebrate reproduction via progesterone receptors...
April 5, 2017: Chemosphere
https://www.readbyqxmd.com/read/28431267/mir-19-targeting-of-gsk3%C3%AE-mediates-sulforaphane-suppression-of-lung-cancer-stem-cells
#18
Jianyun Zhu, Shijia Wang, Yue Chen, Xiaoting Li, Ye Jiang, Xue Yang, Yuan Li, Xiaoqian Wang, Yu Meng, Mingming Zhu, Xiao Ma, Cong Huang, Rui Wu, Chunfeng Xie, Shanshan Geng, Jieshu Wu, Caiyun Zhong, Hongyu Han
Cancer stem cells (CSCs) play a central role in the development of cancer. The canonical Wnt/β-catenin pathway is critical for maintaining stemness of CSCs. Phytochemicals from dietary compounds possess anti-CSCs properties and have been characterized as promising therapeutic agents for the prevention and treatment of many cancers. To date, the involvement and function of miR-19, a key oncogenic miRNA, in regulating Wnt/β-catenin pathway and lung CSCs has not been defined. Meanwhile, the effect of sulforaphane (SFN) on lung CSCs also remains to be elucidated...
April 5, 2017: Journal of Nutritional Biochemistry
https://www.readbyqxmd.com/read/28431223/pink1-based-screen-shines-light-on-autophagy-enhancers-for-parkinson-s-disease
#19
Dominik Haddad, Ken Nakamura
In this issue of Cell Chemical Biology, Zhang et al. (2017) report a zebrafish model of Parkinson's disease (PD), incorporating the PD-protein PINK1 and rotenone, a toxin linked to PD. Using it as a drug-screening platform, they identify trifluoperazine and other piperazine phenothiazines as protective compounds that enhance autophagy independent of PINK1.
April 20, 2017: Cell Chemical Biology
https://www.readbyqxmd.com/read/28431207/syntheses-of-chroman-2-ones-and-%C3%AE-amino-acids-through-a-diastereoselective-domino-reaction
#20
D Balaji Chandrasekhar, Shwu-Chen Tsay, Tapan K Pradhan, Jih Ru Hwu
Many 3-aminochroman-2-ones and β,β-diarylalanines exhibit significant biological activities. A new method was thus developed for the syntheses of these compounds with high efficiency and diastereoselectivity. First, treatment of various phenols with Erlenmeyer-Plochl (Z)-azlactones and AlCl3 in toluene produced the desired cis-3-aminochroman-2-ones in 65-90% yields under kinetic control. This coupling reaction involved a domino process of Friedel-Crafts alkylation, 1,4-AlCl3 shift, transesterification, and protodealumination in a "single-flask...
April 21, 2017: Journal of Organic Chemistry
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