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Showing 1-30 of 45 results for "152757" within Papers
Yakini Brandy et al.
Molecules (Basel, Switzerland), 18(2), 1973-1984 (2013-02-06)
Symmetrical and unsymmetrical 3-halo- or 3-methoxy- substituted 2-dibenzoylamino- 1,4-naphthoquinone analogs were synthesized with an average yield of 45% via sodium hydride promoted bis-acylation of 2-amino-3-chloro-1,4-naphthoquinone, 2-amino-3-bromo-1,4-naphthoquinone and 2-amino-3-methoxy-1,4-naphthoquinone.
Fernanda Luna da Silva et al.
Neurochemistry international, 62(1), 103-112 (2012-10-16)
In the last decades, a series of compounds, including quinones and polyphenols, has been described as having anti-fibrillogenic action on α-synuclein (α-syn) whose aggregation is associated to the pathogenesis of Parkinson's disease (PD). Most of these molecules act as promiscuous
Eduardo Coelho-Cerqueira et al.
Chemical biology & drug design, 83(4), 401-410 (2013-10-30)
Monoamine oxidase (MAO) action has been involved in the regulation of neurotransmitters levels, cell signaling, cellular growth, and differentiation as well as in the balance of the intracellular polyamine levels. Although so far obscure, MAO inhibitors are believed to have
Mozna H Khraiwesh et al.
Archives of pharmacal research, 35(1), 27-33 (2012-02-03)
The antitrypanosomal activities, cytotoxicity, and selectivity indices of eleven imido-substituted 1,4-naphthoquinone derivatives and nifurtimox have been studied. Compared to nifurtimox (IC(50) = 10.67 μM), all the imido-naphthoquinone analogs (IMDNQ1-IMDNQ11) are more potent on Trypanosoma cruzi with IC50 values ranging from
Anita Mahapatra et al.
Bioorganic & medicinal chemistry, 15(24), 7638-7646 (2007-09-25)
The naphthoquinone 7-methyljuglone (5-hydroxy-7-methyl-1,4-naphthoquinone) has previously been isolated and identified as an active component of root extracts of Euclea natalensis which displays antitubercular activity. Herein, a series of synthetic and plant-derived naphthoquinone derivates of the 7-methyljuglone scaffold have been prepared
Shalini John et al.
European journal of medicinal chemistry, 45(9), 4004-4012 (2010-06-29)
Indoleamine 2,3-dioxygenase, a heme-containing enzyme, is emerging as a vital target for the treatment of cancer, chronic viral infections, and other diseases. The aim of this study is to identify novel scaffolds and utilize them in designing potent IDO inhibitors.
Adriano Olímpio da Silva et al.
European journal of medicinal chemistry, 60, 51-56 (2013-01-03)
The discovery and development of essential drugs for Chagas disease is a major concern worldwide. New substituted 1,4-naphthoquinones were synthesized and tested against the infective bloodstream form of Trypanosoma cruzi, the etiological agent of Chagas disease. These products exhibited substantial
Mohankrishna Dalvoy Vasudevarao et al.
The Journal of biological chemistry, 289(11), 7702-7717 (2014-01-29)
Hydroxynaphthoquinone-based inhibitors of the lysine acetyltransferase KAT3B (p300), such as plumbagin, are relatively toxic. Here, we report that free thiol reactivity and redox cycling properties greatly contribute to the toxicity of plumbagin. A reactive 3rd position in the naphthoquinone derivatives
Serena Bertoni et al.
Pharmaceutics, 11(8) (2019-07-31)
The present study aimed to develop a novel formulation containing glutathione (GSH) as an oral antioxidant therapy for the treatment of oxidative stress-related intestinal diseases. To this purpose, solid lipid microparticles (SLMs) with Dynasan 114 and a mixture of Dynasan
Reiko Hirose et al.
The Journal of toxicological sciences, 37(5), 891-898 (2012-10-06)
While metabolic activation of naphthalene, yielding 1,2-naphthoquinone (1,2-NQ) and 1,4-NQ that can covalently bind to cellular proteins, has been recognized to be associated with its toxicity, the current consensus is that such electrophile-mediated covalent modification of sensor proteins with thiolate
Don Antoine Lanfranchi et al.
Organic & biomolecular chemistry, 10(31), 6375-6387 (2012-07-11)
Improving the solubility of polysubstituted 1,4-naphthoquinone derivatives was achieved by introducing nitrogen in two different positions of the naphthoquinone core, at C-5 and at C-8 of menadione through a two-step, straightforward synthesis based on the regioselective hetero-Diels-Alder reaction. The antimalarial
Marianne Placzek et al.
Acta dermato-venereologica, 93(1), 30-32 (2012-09-18)
Benzophenone is a phototoxic compound with absorption maxima in the ultraviolet A (UVA) and ultraviolet B (UVB) range. Many benzophenone derivatives are known to be photosensitizing. On the other hand, 2-hydroxy-4-methoxybenzophenone is used as a photoprotective agent. The aim of
Tomohiro Motono et al.
Journal of separation science, 38(14), 2381-2386 (2015-04-29)
Low-temperature high-performance liquid chromatography, in which a loop injector, column, and detection cell were refrigerated at -35ºC, using liquid carbon dioxide as the mobile phase was developed. Small organic compounds (polyaromatic hydrocarbons, alkylbenzenes, and quinones) were separated by low-temperature high-performance
Olivia Berthoumieu et al.
Chemistry (Weinheim an der Bergstrasse, Germany), 21(36), 12657-12666 (2015-07-17)
Inhibition of the aggregation of the monomeric peptide β-amyloid (Aβ) into oligomers is a widely studied therapeutic approach in Alzheimer's disease (AD). Many small molecules have been reported to work in this way, including 1,4-naphthoquinon-2-yl-L-tryptophan (NQ-Trp). NQ-Trp has been reported
Thasni K A et al.
Molecular carcinogenesis, 52(5), 392-403 (2012-02-01)
It has been shown earlier that plumbagin, a naturally occurring naphthaquinone has specific anticancer activity in BRCA1 blocked ovarian cancer cells. Plumbagin can induce estrogen dependent cell signaling and apoptosis in BRCA1 blocked ovarian cancer cells. Being a reactive oxygen
Julie A Vrana et al.
Toxicological sciences : an official journal of the Society of Toxicology, 140(2), 338-351 (2014-05-16)
The rapid pharmacodynamic response of cells to toxic xenobiotics is primarily coordinated by signal transduction networks, which follow a simple framework: the phosphorylation/dephosphorylation cycle mediated by kinases and phosphatases. However, the time course from initial pharmacodynamic response(s) to cell death
Katarzyna A Broniowska et al.
Biochemistry, 52(25), 4364-4372 (2013-05-31)
When produced at physiological levels, reactive oxygen species (ROS) can act as signaling molecules to regulate normal vascular function. Produced under pathological conditions, ROS can contribute to the oxidative damage of cellular components (e.g., DNA and proteins) and trigger cell
Yoshiyuki Mizushina et al.
International journal of oncology, 42(3), 793-802 (2013-01-23)
Vitamin Ks (VKs) are fat-soluble quinone compounds known to have various bioactivities. This review describes the inflammatory effects of VKs and their related quinone derivatives based on DNA polymerase (pol) inhibition. VK3, but not VK1 or VK2 (=MK-4), inhibited the
Michael G Berg et al.
Molecular and cellular biology, 32(7), 1271-1283 (2012-01-19)
Despite intensive research, there are very few reagents with which to modulate and dissect the mRNA splicing pathway. Here, we describe a novel approach to identify such tools, based on detection of the exon junction complex (EJC), a unique molecular
Ivana Milackova et al.
Journal of enzyme inhibition and medicinal chemistry, 30(1), 107-113 (2014-03-29)
The ability of flavonoids to affect multiple key pathways of glucose toxicity, as well as to attenuate inflammation has been well documented. In this study, the inhibition of rat lens aldose reductase by 3,7-di-hydroxy-2-[4-(2-chloro-1,4-naphthoquinone-3-yloxy)-3-hydroxy-phenyl]-5-hydroxy-chromen-4-one (compound 1), was studied in greater
Yu Shang et al.
Toxicology in vitro : an international journal published in association with BIBRA, 27(2), 922-931 (2013-01-22)
Traffic-related particulate matter (PM) is associated with adverse health effects. Quinones present in the traffic-related PM are hypothesized to contribute to these harmful effects through reactive oxygen species (ROS) generation. However, the impacts of the traffic-related PM and quinones on
Justyna McIntyre et al.
The Journal of biological chemistry, 290(45), 27332-27344 (2015-09-16)
Human DNA polymerases (pols) η and ι are Y-family DNA polymerase paralogs that facilitate translesion synthesis past damaged DNA. Both polη and polι can be monoubiquitinated in vivo. Polη has been shown to be ubiquitinated at one primary site. When
Tianran Sun et al.
Nature communications, 8, 14873-14873 (2017-04-01)
Surface functional groups constitute major electroactive components in pyrogenic carbon. However, the electrochemical properties of pyrogenic carbon matrices and the kinetic preference of functional groups or carbon matrices for electron transfer remain unknown. Here we show that environmentally relevant pyrogenic
David Kokel et al.
Nature chemical biology, 2(6), 338-345 (2006-05-16)
Naphthalene (1) and para-dichlorobenzene (PDCB, 2), which are widely used as moth repellents and air fresheners, cause cancer in rodents and are potential human carcinogens. However, their mechanisms of action remain unclear. Here we describe a novel method for delivering
Oleg Fedorov et al.
Proceedings of the National Academy of Sciences of the United States of America, 104(51), 20523-20528 (2007-12-14)
Protein kinases play a pivotal role in cell signaling, and dysregulation of many kinases has been linked to disease development. A large number of kinase inhibitors are therefore currently under investigation in clinical trials, and so far seven inhibitors have
Dianne Lim et al.
Journal of chromatography. B, Analytical technologies in the biomedical and life sciences, 879(30), 3592-3598 (2011-10-26)
A method was developed for the quantification of 1-4 ring quinones in urine samples using liquid-liquid extraction followed by analysis with gas chromatography-mass spectrometry. Detection limits for the ten quinones analyzed are in the range 1-2 nmol dm(-3). The potential
Paula F Carneiro et al.
Bioorganic & medicinal chemistry, 20(16), 4995-5000 (2012-07-17)
New oxirane derivatives were synthesized using six naphthoquinones as the starting materials. Our biological results showed that these oxiranes acted as trypanocidal agents against Trypanosoma cruzi with minimal cytotoxicity in the VERO cell line compared to naphthoquinones. In particular, oxirane
S Pushpam et al.
Spectrochimica acta. Part A, Molecular and biomolecular spectroscopy, 114, 272-276 (2013-06-19)
The dependence of fluorescence emission of 2-amino-3-bromo-1,4-naphthoquinone on titanium dioxide (TiO2) in methanol has been investigated. The increase in TiO2 concentration causes a decrease in the fluorescence intensity of 2-amino-3-bromo-1,4-naphthoquinone. A linear Stern-Volmer plot in this study indicates the presence
Daniela M Santos et al.
Molecular neurobiology, 47(1), 313-324 (2012-10-12)
Naphthoquinones are bioactive compounds widespread in nature that impact on several cellular pathways, including cell proliferation and survival, by acting as prooxidants and electrophiles. We have previously described the role of the synthetic isoxazole condensed 1,4-naphthoquinone derivative 1a in preventing
Sanjeev Kumar et al.
Journal of medicinal chemistry, 51(6), 1706-1718 (2008-03-06)
Indoleamine 2,3-dioxygenase (IDO) is emerging as an important new therapeutic target for the treatment of cancer, chronic viral infections, and other diseases characterized by pathological immune suppression. While small molecule inhibitors of IDO exist, there remains a dearth of high-potency
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