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https://www.readbyqxmd.com/read/27921386/cytotoxicity-of-a-series-of-norcantharidin-inspired-tetrahydroepoxyisoindole-carboxamides
#1
Christopher Peter Gordon, Lawson K Spare, Pasquale Falsetta, Jayne Gilbert, David G Harman, Mark A Baker, Feng Li, Adam McCluskey, Jack K Clegg, Jennette A Sakoff, Janice R Aldrich-Wright
A series of 28 norcantharidin (NorC) inspired analogues were accessed via a robust two-step Ugi intramolecular Diels-Alder (IMDA) sequence. Four analogues displayed equipotent whole cell cytotoxicity to NorC and cisplatin against a number of cancer cell lines and a normal breast cell line (MCF10A). Notably (3S,3aS,6R)-2-benzyl-7-methyl-N-(naphthalen-2-yl)-1-oxo-1,2,3,6-tetrahydro-3a,6-epoxyisoindole-3-carboxamide (trans-27) displayed superior whole cell activity against breast (MCF-7, GI50 = 2.9 µM) and colon (HT29, GI50 = 6...
December 6, 2016: ChemMedChem
https://www.readbyqxmd.com/read/27914800/discovery-of-a-new-isomannide-based-peptidomimetic-synthetized-by-ugi-multicomponent-reaction-as-human-tissue-kallikrein-1-inhibitor
#2
Thalita G Barros, Jorge A N Santos, Bruno E G de Souza, Ana Carolina R Sodero, Alessandra M T de Souza, Dayane P da Silva, Carlos Rangel Rodrigues, Sergio Pinheiro, Luiza R S Dias, Bárbara Abrahim-Vieira, Luciano Puzer, Estela M F Muri
Human kallikrein 1 (KLK1) is the most extensively studied member of this family and plays a major role in inflammation processes. From Ugi multicomponent reactions, isomannide-based peptidomimetic 10 and 13 where synthesized and showed low micromolar values of IC50 for KLK1 The most active compound (10) presented competitive mechanism, with three structural modifications important to interact with active site residues which corroborates its KLK1 inhibition. Finally, the most active compound also showed good ADMET profile, which indicates compound 10 as a potential hit in the search for new KLK1 inhibitors with low side effects...
November 18, 2016: Bioorganic & Medicinal Chemistry Letters
https://www.readbyqxmd.com/read/27910982/synthesis-of-6-methyl-3-4-dihydropyrazinones-using-an-ugi-4-cr-allenamide-cycloisomerization-protocol
#3
Estefanía Icelo-Ávila, Yoarhy A Amador-Sánchez, Luis A Polindara-García, Luis D Miranda
A synthetic approach to the 6-methyl-3,4-dihydropyrazinone core from Ugi adducts is described. This methodology relies on the regioselective C-N bond formation between an allenamide moiety at C-β and an amide anion formed under base-mediated conditions. This protocol allows easy access to tricyclic systems such as pyrazino[2,1-a]isoindole and pyrazino[2,1-a]isoquinoline nuclei.
December 2, 2016: Organic & Biomolecular Chemistry
https://www.readbyqxmd.com/read/27898350/cronkhite-canada-syndrome-complicated-by-pulmonary-embolism-a-case-report
#4
Neha L Nemade, Urvi B Shukla, Gajanan D Wagholikar
INTRODUCTION: Cronkhite Canada Syndrome (CCS) is a rare syndrome, described in 1955 by Americans, Leonard Wolsey Cronkhite and Wilma Jeanne Canada in the New England Journal of Medicine [1]. About 450 cases have been reported. Complications, like malignant transformation, unprovoked thromboembolism is known. Since there is wide variability in medical presentation, no definitive diagnostic and treatment protocol s have been set. The mortality remains at 55%. CASE PRESENTATION: We report a case of a 50 year old male patient presenting with diarrhea, weight loss, abdominal pain, ectodermal features...
November 17, 2016: International Journal of Surgery Case Reports
https://www.readbyqxmd.com/read/27878155/spin-labelled-diketopiperazines-and-peptide-peptoid-chimera-by-ugi-multi-component-reactions
#5
Haider N Sultani, Haleh H Haeri, Dariush Hinderberger, Bernhard Westermann
For the first time, spin-labelled coumpounds have been obtained by isonitrile-based multi component reactions (IMCRs). The typical IMCR Ugi-protocols offer a simple experimental setup allowing structural variety by which labelled diketopiperazines (DKPs) and peptide-peptoid chimera have been synthesized. The reaction keeps the paramagnetic spin label intact and offers a simple and versatile route to a large variety of new and chemically diverse spin labels.
November 23, 2016: Organic & Biomolecular Chemistry
https://www.readbyqxmd.com/read/27869255/metal-catalyzed-c-h-functionalization-involving-isocyanides
#6
REVIEW
Bingrui Song, Bin Xu
Isocyanides have a broad range of applications in multicomponent reactions such as Passerini and Ugi processes. Recent advances in metal catalysis have tremendously increased the versatility of isocyanides in organic chemistry. Suitable metal catalysts could selectively activate various C-H bonds to allow direct functionalization under mild conditions, which represents a chemical process with broad synthetic potential. The synergy from the combination of isocyanide insertion and C-H bond activation offers an efficient and powerful tool to establish complicated reactions and to construct useful substances, from which the high potential of such strategy has been convincingly demonstrated in drug discovery, organic synthesis, and materials science...
November 21, 2016: Chemical Society Reviews
https://www.readbyqxmd.com/read/27848201/the-role-of-hemoglobin-laboratory-test-results-for-the-detection-of-upper-gastrointestinal-bleeding-outcomes-resulting-from-the-use-of-medications-in-observational-studies
#7
Elisabetta Patorno, Joshua J Gagne, Christine Y Lu, Kevin Haynes, Andrew T Sterrett, Jason Roy, Xingmei Wang, Marsha A Raebel
INTRODUCTION: The identification of upper gastrointestinal (UGI) bleeding and perforated ulcers in claims data typically relies on inpatient diagnoses. The use of hemoglobin laboratory results might increase the detection of UGI events that do not lead to hospitalization. OBJECTIVES: Our objective was to evaluate whether hemoglobin results increase UGI outcome identification in electronic databases, using non-steroidal anti-inflammatory drugs (NSAIDs) as a test case...
November 15, 2016: Drug Safety: An International Journal of Medical Toxicology and Drug Experience
https://www.readbyqxmd.com/read/27833405/efficacy-of-retrievable-metallic-stent-with-fixation-string-for-benign-stricture-after-upper-gastrointestinal-surgery
#8
Jeong-Eun Kim, Hyo-Cheol Kim, Myungsu Lee, Saebeom Hur, Minuk Kim, Sang Hwan Lee, Soo Buem Cho, Chan Sun Kim, Joon Koo Han
OBJECTIVE: To determine the efficacy of retrievable metallic stent with fixation string for benign anastomotic stricture after upper gastrointestinal (UGI) surgery. MATERIALS AND METHODS: From June 2009 to May 2015, a total of 56 retrievable metallic stents with fixation string were placed under fluoroscopy guidance in 42 patients who were diagnosed with benign anastomotic stricture after UGI surgery. Clinical success was defined as achieving normal regular diet (NRD)...
November 2016: Korean Journal of Radiology: Official Journal of the Korean Radiological Society
https://www.readbyqxmd.com/read/27829908/application-of-heterocyclic-aldehydes-as-components-in-ugi-smiles-couplings
#9
Katelynn M Mason, Michael S Meyers, Abbie M Fox, Sarah B Luesse
Efficient one-pot Ugi-Smiles couplings are reported for the use of furyl-substituted aldehyde components. In the presence of these heterocyclic aldehydes, reactions tolerated variations in amine components and led to either isolated N-arylamide Ugi-Smiles adducts or N-arylepoxyisoindolines, products of tandem Ugi-Smiles Diels-Alder cyclizations, in moderate yields. A thienyl-substituted aldehyde was also a competent component for Ugi-Smiles adduct formation.
2016: Beilstein Journal of Organic Chemistry
https://www.readbyqxmd.com/read/27812289/concentrations-of-water-soluble-vitamins-in-blood-and-urinary-excretion-in-patients-with-diabetes-mellitus
#10
Hiromi Iwakawa, Yasuyuki Nakamura, Tomiho Fukui, Tsutomu Fukuwatari, Satoshi Ugi, Hiroshi Maegawa, Yukio Doi, Katsumi Shibata
We examined the concentrations of water-soluble vitamins in blood and urinary excretion of 22 patients with type 2 diabetes mellitus (type 2DM) and 20 healthy control participants. Macronutrient and vitamin intakes of type 2DM subjects were measured using a weighed food record method. Control participants consumed a semipurified diet for eight days. Multiple linear regression models were used to determine whether significant differences existed in vitamin concentrations in blood independent of age, sex, and other confounding factors...
2016: Nutrition and Metabolic Insights
https://www.readbyqxmd.com/read/27811012/her2-status-in-advanced-or-metastatic-gastric-esophageal-or-gastro-esophageal-adenocarcinoma-for-entry-to-the-trio-013-logic-trial-of-lapatinib
#11
Michael F Press, Catherine E Ellis, Robert C Gagnon, Tobias J Grob, Marc Buyse, Ivonne Villalobos, Zhiyong Liang, Shafei Wu, Yung-Jue Bang, Shu-Kui Qin, Hyun Cheol Chung, Jianming Xu, Joon Oh Park, Krzysztof Jeziorski, Karen Afenjar, Yanling Ma, Monica C Estrada, Douglas M Robinson, Stefan J Scherer, Guido Sauter, J Randolph Hecht, Dennis J Slamon
HER2/ERBB2 status is used to select patients for HER2-targeted therapy. HER2/ERBB2 amplification/overexpression of upper gastrointestinal (UGI) adenocarcinomas was determined locally or in two central laboratories to select patients for the TRIO-013/LOGiC trial of chemotherapy with or without lapatinib. Patients selected locally had central laboratory confirmation of HER2-amplification for inclusion in the primary efficacy population. HER2 was assessed with PathVysion or IQ PharmDx fluorescence in situ hybridization (FISH) and HercepTest immunohistochemistry assays...
November 3, 2016: Molecular Cancer Therapeutics
https://www.readbyqxmd.com/read/27806030/a-morbidity-mortality-analysis-of-a-tertiary-level-upper-gastrointestinal-hepatopancreaticobiliary-surgical-unit
#12
Susrutha K Wickremesekera, Ho Beom Sean Seo, Mary Anne Trimber, Simon Bann, Katherine Tse
: Internationally, regionalisation of major upper gastrointestinal/hepatopancreaticobiliary (UGI/HPB) surgery to a selected number of expert hospital centres has demonstrated that high hospital volume is associated with lower mortality and morbidity. The Wellington UGI/HPB unit compared to international institutions is a low volume unit, however within New Zealand we perform a high number of Upper GI/HPB cases. AIMS: The aim of this study was to evaluate the quality measures of morbidity and mortality of major upper gastrointestinal and hepatopancreatobiliary surgeries performed at the Wellington UGI/HPB unit...
October 28, 2016: New Zealand Medical Journal
https://www.readbyqxmd.com/read/27785312/nodule-regression-in-adults-with-nodular-gastritis
#13
Ji Wan Kim, Sun-Young Lee, Jeong Hwan Kim, In-Kyung Sung, Hyung Seok Park, Chan-Sup Shim, Hye Seung Han
BACKGROUND: Nodular gastritis (NG) is associated with the presence of Helicobacter pylori infection, but there are controversies on nodule regression in adults. The aim of this study was to analyze the factors that are related to the nodule regression in adults diagnosed as NG. METHODS: Adult population who were diagnosed as NG with H. pylori infection during esophagogastroduodenoscopy (EGD) at our center were included. Changes in the size and location of the nodules, status of H...
December 2015: Gastroenterology Research
https://www.readbyqxmd.com/read/27777842/regioselective-synthesis-of-a-family-of-%C3%AE-lactams-bearing-a-triazole-moiety-as-potential-apoptosis-inhibitors
#14
Maria Garrido, Miriam Corredor, Mar Orzáez, Ignacio Alfonso, Angel Messeguer
Apoptosis is a biological process important to several human diseases; it is strongly regulated through protein-protein interactions and complex formation. We previously reported the synthesis of apoptosis inhibitors bearing an exocyclic triazole amide isoster by using an Ugi four-component coupling reaction (Ugi-4CC), followed by a base-promoted intramolecular cyclization. Depending on the substitution patterns and the reaction conditions, this cyclization forms the six- or four-membered ring. Two compounds bearing the β-lactam scaffold turned out to be the most potent inhibitors...
October 2016: ChemistryOpen
https://www.readbyqxmd.com/read/27773392/tryptophan-tags-and-de-novo-designed-complementary-affinity-ligands-for-the-expression-and-purification-of-recombinant-proteins
#15
Ana Sofia Pina, Sara Carvalho, Ana Margarida G C Dias, Márcia Guilherme, Alice S Pereira, Luciana T Caraça, Ana Sofia Coroadinha, Christopher R Lowe, A Cecília A Roque
A common strategy for the production and purification of recombinant proteins is to fuse a tag to the protein terminal residues and employ a "tag-specific" ligand for fusion protein capture and purification. In this work, we explored the effect of two tryptophan-based tags, NWNWNW and WFWFWF, on the expression and purification of Green Fluorescence Protein (GFP) used as a model fusion protein. The titers obtained with the expression of these fusion proteins in soluble form were 0.11mgml(-1) and 0.48mgml(-1) for WFWFWF and NWNWNW, respectively...
October 19, 2016: Journal of Chromatography. A
https://www.readbyqxmd.com/read/27770934/structural-and-rheological-characterizations-of-nanoparticles-of-environment-sensitive-hydrophobic-alginate-in-aqueous-solution
#16
Kai Chen, Jiacheng Li, Yuhong Feng, Furui He, Qingfeng Zhou, Dunchao Xiao, Yiyuan Tang
Amphiphilic polymers that form self-assembled structures in aqueous media have been investigated and used for the diagnosis and therapy of various diseases, including cancer. In our work, a series of environment-sensitive hydrophobic alginates (Ugi-Alg) with various weight-average molecular mass values (Mw~6.7×10(5)-6.7×10(4)g/mol) were synthesized via Ugi reaction. The structure of Ugi-Alg was characterized by (1)HNMR spectrometer. The electrostatic self-assembly of different molecular weight (Mw) and composition (M/G ratio) of Ugi-Alg chain under various Na(+) concentrations, was investigated by dynamic light scattering, electron spin resonance experiments, and transmission electron microscopy...
January 1, 2017: Materials Science & Engineering. C, Materials for Biological Applications
https://www.readbyqxmd.com/read/27749981/etiology-and-outcome-in-patients-with-upper-gastrointestinal-bleeding-study-on-4747-patients-in-the-central-region-of-iran
#17
Mohammad Minakari, Shervin Badihian, Pooyan Jalalpour, Vahid Sebghatollahi
BACKGROUND AND AIM: Upper gastrointestinal bleeding (UGIB) is a threatening condition leading to urgent hospitalization. This study aims to investigate etiology and outcome in UGIB patients in Iran. METHODS: Medical records of GIB patients admitted to Alzahra referral hospital (in Isfahan) during 2010-2015 were retrospectively reviewed for demographic data, comorbidities, history of smoking and taking non-steroidal anti-inflammatory drugs (NSAIDs), presenting symptoms, endoscopic findings, therapeutic endoscopy, blood products' infusion, surgical intervention and mortality...
October 17, 2016: Journal of Gastroenterology and Hepatology
https://www.readbyqxmd.com/read/27739136/bariatric-surgery-and-type-2-diabetes-are-there-weight-loss-independent-therapeutic-effects-of-upper-gastrointestinal-bypass
#18
M Chondronikola, L L S Harris, S Klein
Type 2 diabetes (T2D) is a major worldwide public health concern. Despite a large armamentarium of T2D medications, a large proportion of patients fail to achieve recommended treatment goals for glycemic control. Weight loss has profound beneficial effects on the metabolic abnormalities involved in the pathogenesis of T2D. Accordingly, bariatric surgery, which is the most effective available weight loss therapy, is also the most effective therapy for treating patients with T2D. Surgical procedures that bypass the upper gastrointestinal (UGI) tract are particularly effective in achieving partial and even complete remission of T2D, suggesting that UGI bypass has weight loss-independent effects on glycemic control...
November 2016: Journal of Internal Medicine
https://www.readbyqxmd.com/read/27736941/a-novel-class-of-small-molecule-agonists-with-preference-for-human-over-mouse-tlr4-activation
#19
Jason D Marshall, Darren S Heeke, Eileen Rao, Sean K Maynard, David Hornigold, Christopher McCrae, Neil Fraser, Andrey Tovchigrechko, Li Yu, Nicola Williams, Sarah King, Martin E Cooper, Adeline M Hajjar, Jennifer C Woo
The best-characterized Toll-like receptor 4 (TLR4) ligands are lipopolysaccharide (LPS) and its chemically modified and detoxified variant, monophosphoryl lipid A (MPL). Although both molecules are active for human TLR4, they demonstrate a potency preference for mouse TLR4 based on data from transfected cell lines and primary cells of both species. After a high throughput screening process of small molecule libraries, we have discovered a new class of TLR4 agonist with a species preference profile differing from MPL...
2016: PloS One
https://www.readbyqxmd.com/read/27736061/the-antioxidant-additive-approach-for-alzheimer-s-disease-therapy-new-ferulic-lipoic-acid-plus-melatonin-modified-tacrines-as-cholinesterases-inhibitors-direct-antioxidants-and-nuclear-factor-erythroid-derived-2-like-2-activators
#20
Mohamed Benchekroun, Alejandro Romero, Javier Egea, Rafael León, Patrycja Michalska, Izaskun Buendia, Maria Luisa Jimeno, Daniel Jun, Jana Janockova, Vendula Sepsova, Ondrej Soukup, Oscar M Bautista-Aguilera, Bernard Refouvelet, Olivier Ouari, José Marco-Contelles, Lhassane Ismaili
Novel multifunctional tacrines for Alzheimer's disease were obtained by Ugi-reaction between ferulic (or lipoic acid), melatonin, formaldehyde, and tacrine derivatives, according to the antioxidant additive approach in order to modulate the oxidative stress as therapeutic strategy. Compound 5c has been identified as a promising permeable agent showing excellent antioxidant properties, strong cholinesterase inhibitory activity, less hepatotoxicity than tacrine, and the best neuroprotective capacity, being able to significantly activate the Nrf2 transcriptional pathway...
October 13, 2016: Journal of Medicinal Chemistry
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