Abstract
The FT-IR and the high resolution (1)H and (13)C NMR spectra have been recorded for N'-(2-methyl-3-phenylallylidene)nicotinohydrazide (1) and N'-(2-methyl-3-phenylallylidene)isonicotinohydrazide (2) and analyzed. (1)H-(1)H COSY spectra were also recorded for the hydrazides. The spectral studies reve...
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PMID: 20638897
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Abstract
We show that the concentration-dependent use of salen-manganese complexes within the appropriate time window and with parallel control of signaling parameters allows complex interactions during intercellular induction of apoptosis to be studied. At very low concentrations, salen-manganese complexes...
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PMID: 21036710
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Abstract
We for the first time report the role of ecdysteroids in the regulation of hexamerin synthesis in a lepidopteran insect Corcyra cephalonica. The hormonal studies were carried out using the normal and the thorax-ligated insects with both 20E and its non-steroidal agonist RH-5992. The in vitro as well...
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PMID: 20361975
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Abstract
Thiol (-SH) groups were introduced into unfractionated heparin by reaction of carboxyl groups in its uronic acid residues with 3,3'dithiobis(propanoic)hydrazide. Thiolated heparin derivatives were then linked to pyridyl disulfide-activated polyethylene oxide-polypropylene oxide-polyethylene oxide tr...
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PMID: 20621768
PDF is available here.
Abstract
We demonstrate for the first time the applicability of fluorescence lifetime correlation spectroscopy (FLCS) to monitor the interaction of an antagonist antibody with the epidermal growth factor receptor (EGFR) in live cells. As a proof of concept, we demonstrate the interaction of Cy5 labeled IgG a...
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PMID: 20586411
PDF is available here.
Abstract
The stimulated exocytotic release of ET-1 is dramatically increased in aged endothelium. This reflects increased reactivity of exocytosis, increased expression and storage of ET-1 precursor peptides, and increased expression of ECE-1. Altered endothelial exocytosis of ET-1 and other mediators may co...
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PMID: 20522806
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Abstract
We wanted to understand the significance of induction of ERRgamma expression in skeletal muscle by exercise. Muscle-specific VP16ERRgamma transgenic mice demonstrated an increase in exercise capacity, mitochondrial enzyme activity, and enlarged mitochondria despite lower muscle weights. Furthermore,...
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PMID: 20418374
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Abstract
The influence of protein oxidation, as measured by the dinitrophenylhydrazine (DNPH) method, on colour and texture changes during chill storage (2 degrees C, 12days) of cooked burger patties was studied. Extracts from arbutus-berries (Arbutus unedoL., AU), common hawthorns (Crataegus monogynaL., CM)...
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PMID: 20416800
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Abstract
We found that MDA19 exhibited a distinctive in vitro functional profile at rat CB2 receptors and behaved as a CB1/CB2 agonist in vivo, characteristics of a protean agonist. MDA19 has potential for alleviating neuropathic pain without producing adverse effects in the central nervous system....
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PMID: 20522703
PDF is available here.
Abstract
We conducted a phase I translational study to evaluate the toxicities and estimate the maximum tolerated dose (MTD) of laromustine when administered with temozolomide (TMZ) in patients with hematologic malignancies.
TMZ was delivered twice daily for 5 doses followed by a single infus...
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PMID: 20511167
PDF is available here.
Abstract
The reaction of 3beta-hydroxy-21-hydroxymethylidenepregn-5-en-3beta-ol-20-one (1) with phenylhydrazine (2a) affords two regioisomers, 17beta-(1-phenyl-3-pyrazolyl)androst-3-en-3beta-ol (5a) and 17beta-(1-phenyl-5-pyrazolyl)androst-5-en-3beta-ol (6a). The direction of the ring-closure reactions of 1...
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PMID: 20206195
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Abstract
We concluded that the lethal and sublethal effects of methoxyfenozide are likely to have a significant impact on S. exigua populations on treated crops....
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PMID: 20568611
PDF is available here.
Abstract
We describe the action of AF-2364 on human sperm in vitro, as well as the mechanisms involved. AF-2364 specifically blocked human sperm motility in vitro. Further experiments revealed that AF-2364 can target sperm mitochondrial permeability transition (MPT) pores to induce the loss of sperm mitochon...
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PMID: 20418891
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Abstract
MR relaxometry revealed a dose-dependent binding of T84.1-conjugated SPIO particles with a positive correlation between R(2) relaxation rate of cell samples and SPIO particle concentration during incubation (r=0.993, P<.01). Positive correlations were also observed between R(2) relaxation rate and f...
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PMID: 20117898
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Abstract
New approaches for the synthesis of hydrazide-hydrazone derivatives were demonstrated as well as some heterocyclizations of such derivatives to afford 1,3,4-triazine, pyridine and 1,3,4-oxadiazine derivatives. The antitumor evaluation of the newly synthesized products against three cancer cell lines...
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PMID: 20657502
PDF is available here.
Abstract
A novel fluorescence turn-on method for sensitive and selective detection of protamine was developed based on aggregation-induced emission enhancement (AIEE) characteristics of 4-(6'-carboxyl)hexyloxysalicylaldehyde azine (CHSA) induced by electrostatic interaction between protamine and CHSA(-). Und...
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PMID: 20419262
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Abstract
Small molecules inhibiting hypoxia inducible factor (HIF) prolyl hydroxylases (PHDs) are the focus of drug development efforts directed toward the treatment of ischemia and metabolic imbalance. A cell-based reporter produced by fusing HIF-1 alpha oxygen degradable domain (ODD) to luciferase was show...
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PMID: 20416509
PDF is available here.
Abstract
Methyl indolenines (4a-c) and(5a-c) were prepared in high yield by a Fischer indole synthesis reaction of o,m-tolylhydrazine hydrochlorides (1a-b) with isopropyl methyl ketone (2) and 2-methylcyclohexanone (3) in acetic acid at room temperature. o,p- Nitrophenylhydrazines (1c-d) were reacted with 2-...
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PMID: 20428058
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Abstract
A novel fluorescence turn-on detection method of human serum albumin (HSA) and bovine serum albumin (BSA) in aqueous solution is investigated using 2,4-dihydroxyl-3-iodo salicylaldehyde azine (DISA). Upon the addition of DISA to HSA/BSA solution, a fluorescence turn-on effect at 529 nm can be observ...
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PMID: 20152438
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Abstract
Au nanoparticle (nAu) based electrochemical platform for the amperometric sensing of isoniazid at sub-nanomolar level is developed. The sol-gel derived 3-dimensional silicate network pre-assembled on a conducting substrate is chemically decorated with nAu of 70-100 nm by seed-mediated growth approac...
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PMID: 20152392
PDF is available here.
Abstract
A series of N-mustard-quinoline conjugates bearing a urea or hydrazinecarboxamide linker was synthesized for antitumor evaluation. The in vitro cytotoxicity studies revealed that compounds with hydrazinecarboxamide linkers were generally more cytotoxic than the corresponding urea counterparts in inh...
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PMID: 20181487
PDF is available here.
Abstract
Bacteria and higher plants make l-lysine from diaminopimelic acid (DAP). In mammals l-lysine is an essential amino acid that must be acquired from the diet as the biosynthetic pathway is absent for this key constituent of proteins. Recently, ll-diaminopimelate aminotransferase (ll-DAP-AT), a pyridox...
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PMID: 20185317
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Abstract
Immunosuppressants, erythropoiesis-stimulating agents in combination with granulocyte colony-stimulating factor or all-trans-retinoic-acid have shown improvement in decreasing the need for transfusions and improving quality-of-life and/or survival. Eltrombopag has shown promising results in the trea...
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PMID: 20178141
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Abstract
IMPORTANCE OF THE FIELD: In spite of the recent progress, the prognosis of acute myelogenous leukemia (AML) remains poor, particularly in patients with relapsed disease and in the elderly. In these situations, there is at present no standard of care, and new drugs are urgently needed. AREAS COVERED...
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PMID: 20163276
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Abstract
We report the deacylation of (20R)-20-acetyl-23,24-dinorcholanic lactones by hydrazine hydrate, under microwave irradiation in high yields. The elimination of the 20-acetyl group proceeded with retention of configuration which contrast with other proved deacylation methods that yield a mixture of di...
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PMID: 20034505
PDF is available here.
Abstract
We demonstrate that ERRbeta is transiently induced, and ERRgamma is dramatically induced (and accumulates) in a differentiation-dependent manner in skeletal muscle cells. Treatment of differentiated skeletal muscle cells with the ERRbeta/gamma agonist (GSK4716) produced a significant increase in the...
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PMID: 19631715
PDF is available here.
Abstract
We use antipeptide antibodies to peptides corresponding to the FSHR-ELs to check the surface accessibility of the loops. These antibodies were further used to understand the involvement of the loops in hormone binding and signaling. The results demonstrate that EL1 and EL3 are surface accessible on...
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PMID: 19825393
PDF is available here.
Author(s) unavailable
Abstract
When corticosteroid therapy, immunoglobulin and splenectomy fail to control chronic idiopathic thrombocytopenic purpura and the risk of bleeding remains high, romiplostim is an acceptable option but close monitoring is needed to evaluate long-term risks. Eltrombopag (Revolade, GlaxoSmithKline) is a...
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PMID: 20455333
PDF is available here.
Abstract
Thrombocytopenia is a common clinical problem in HCV-infected cases. Multiple studies have consistently shown a rise in platelet count following a successful HCV treatment thus proving a cause-effect relationship between the two. Although, many therapeutic strategies have been tried in the past to t...
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PMID: 20065578
PDF is available here.
Abstract
A new ligand, (E)-N'-[1-(pyridin-2-yl)ethylidene]isonicotinohydrazide (HL), was prepared by condensation of 2-acetylpyridine and isonicotinohydrazide in ethanol. Its two lanthanide(III) complexes, [Nd(III)(L)(2)(NO(3))(CH(3)OH)(2)]·CH(3)CH(2)OH (1), and [Pr(III)(L)(2)(NO(3))(CH(3)OH)(2)]·CH(3)CH(2...
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PMID: 20930395
PDF is available here.
Abstract
I (SVPD), whereas oxovanadium(IV) complexes of these ligands show varying degrees of inhibition and are found to be non-competitive inhibitors. The superoxide and nitric oxide radical scavenging properties have been determined. Hydrazide ligands are inactive against these free radicals, whereas thei...
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PMID: 19912066
PDF is available here.
Abstract
With properly encoded recognition sites and a well-defined algorithm for intermolecular and intramolecular interactions, the 120 degrees spacer linked ditopic hydrazide-based supramolecular synthons were found to self-assemble into shape-persistent cyclic hexamers in apolar solvents. The two hydrazi...
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PMID: 19685881
PDF is available here.
Abstract
We designed a series of small-molecule ligands derived from a known ERRgamma agonist, GSK4716, that can substantially potentiate the transcriptional activity of ERRgamma. Individual compounds among a 30-member library of acyl hydrazones were pre-evaluated through in silico docking studies on the rec...
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PMID: 19746993
PDF is available here.
Abstract
It has been shown that ITP is not purely due to platelet destruction, and in a significant proportion platelet production is suboptimal. Further interest developed with the discovery that the recombinant thrombopoietins (TPOs) could enhance platelet production in a variety of thrombocytopenic states...
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PMID: 19553811
PDF is available here.
Abstract
I collagen and is a target for the pharmacological treatment of osteoporosis. Further roles for Cat K have been recently described, some of which are supported by the use of purportedly selective Cat K inhibitors in human and rodent cell-based assays. Twelve commercial and non-commercial Cat K inhib...
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PMID: 19453281
PDF is available here.
Abstract
A simple, new three-step sequence for the conversion of hydrazides into pyridines is reported in which the key steps are N-H insertion by a copper carbene intermediate derived from alpha-diazo-beta-ketoesters into the hydrazide, reaction with ammonium acetate to give 1,2,4-triazines, followed by Die...
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PMID: 19719202
PDF is available here.
Abstract
A novel ratiometric Raman spectroscopic (RMRS) method has been developed for quantitative determination of protein carbonyl levels. Oxidized bovine serum albumin (BSA) and oxidized lysozyme were used as model proteins to demonstrate this method. The technique involves conjugation of protein carbonyl...
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PMID: 19457432
PDF is available here.
Abstract
We oxidized the carbohydrates of secreted proteins and those on the cell surface with periodate and isolated them via covalent coupling to hydrazide resin. The glycoproteins obtained were identified from tryptic peptides and N-linked glycopeptides released from the hydrazide resin using two-dimensio...
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PMID: 19530676
PDF is available here.
Abstract
In the seminiferous epithelium, Eps8 is localized to actin-based cell junctions at the blood-testis barrier (BTB) and the apical ectoplasmic specialization (ES) in stage V-VI tubules but is considerably diminished in stage VIII tubules. Eps8 down-regulation coincides with the time of BTB restructuri...
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PMID: 19293393
PDF is available here.
Abstract
Effects on adult longevity, fecundity and fertility, as well as long-term effects on progeny were determined through oral exposure of Spodoptera littoralis (Boisduval) (Lepidoptera: Noctuidae) adults to azadirachtin and methoxyfenozide. Both compounds reduced adult longevity by 2.3 d at the higher c...
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PMID: 19736761
PDF is available here.
Abstract
A fluorimetric detection method for one of the tryptophan metabolites, cinnabarinic acid (CA), which has recently been reported to have the ability to induce apoptosis in thymocytes, was developed using o-tolyl hydrazine (TH) as the derivatization reagent. The carbonyl group at posit...
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PMID: 19630072
PDF is available here.
Abstract
2-Hydrazinyl-1,4,5,6-tetrahydropyrimidin-5-ol dihydrochloride 2, as well as 2-hydrazinyl-4,5-dihydro-1H-imidazole dihydrochloride 1, was synthesized as metal-free DNA cleaving agent. Agarose gel electrophoresis was used to assess the plasmid pUC 19 DNA cleavage activities in the pres...
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PMID: 19481940
PDF is available here.
Abstract
The effects of NO on NR activity in tomato roots depend on levels of nitrate supply, and probably result from direct interactions between NO and NR protein....
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PMID: 19376780
PDF is available here.
Abstract
Recent studies suggested an involvement of thromboxane A2 in cyclooxygenase-2-dependent inhibition of steroidogenic acute regulatory (StAR) gene expression. The present study further investigated the role of thromboxane A2 receptor in StAR gene expression and steroidogenesis in testicular Leydig cel...
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PMID: 19325001
PDF is available here.
Abstract
We tested the hypothesis that vascular dysfunction may be due to altered expression and activity of these effectors of NO signaling. Every other set of rat second order mesenteric resistance arteries (MA) were ligated, resulting in chronic low flow (LF) in the upstream MA1 and high flow (HF) in the...
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PMID: 19374906
PDF is available here.
Abstract
A 4-week course of rituximab is associated with a platelet count response in 60% of patients with ITP, and durable responses have been observed. Subtle increases in infection have been reported. Romiplostim and eltrombopag are each associated with a 60 - 85% response while on treatment. Transient bo...
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PMID: 19426124
PDF is available here.
Abstract
An indole-azadiene conjugate (1), synthesized by facile one-step condensation, behaves as a highly selective probe for detection of fluoride ion both in colorimetric and fluorometric analyses. The probe 1 shows F(-)-selective color change from colorless to yellow and appearance of green fluorescence...
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PMID: 19421444
PDF is available here.
Abstract
We designed and synthesized a series of pyrroloquinoxaline compounds with hydrazine moiety linking a nitrogen-containing polycyclic group to a heteroaroyl system. Several derivatives, with attractive drug-like properties, were identified as promising cytotoxic agents, showing excellent potency in a...
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PMID: 19388873
PDF is available here.
Abstract
JS-118 is a diacylhydrazines-type insect growth regulator which is now used extensively in China. The hydrolysis and photolysis of the pesticide JS-118 in aqueous solutions have been assessed under natural and controlled conditions in this project. Hydrolysis experimental results show that JS-118 is...
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PMID: 19165405
PDF is available here.
Abstract
Fluorescence techniques can provide insights into the environment of fluorescent indicators incorporated within a ligand as it is bound to its receptor. Fluorescent indicators of different sizes and chemical characteristics ranging from hydrophilic to hydrophobic that are incorporated into a recepto...
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PMID: 19513657
PDF is available here.
Abstract
We described a series of salicylhydrazide compounds with potent anti-cancer activities against a panel of human cancer cell lines derived from different origins. Preclinical evaluation showing efficacy both in vitro and in vivo in human cancer models indicated that these agents may represent a promi...
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PMID: 19275759
PDF is available here.
Abstract
We described a series of salicylhydrazide compounds with potent anti-cancer activities against a panel of human cancer cell lines derived from different origins. Preclinical evaluation showing efficacy both in vitro and in vivo in human cancer models indicated that these agents may represent a promi...
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PMID: 19275759
PDF is available here.
Abstract
We discovered a novel class of salicylhydrazide compounds with remarkable activity in hormone-dependent and -independent human cancer cells. We then designed and synthesized numerous analogues. Among these analogues, a quinoxalinhydrazide compound, SC144, exhibited desirable physicochemical and drug...
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PMID: 19221468
PDF is available here.
Abstract
Chronic Immune Thrombocytopenic Purpura (cITP) has become a field of multiple therapeutic assays. More than 20 types of treatment have been developed to obtain a favorable and prolonged platelet response. The treatment of cITP is oriented to inhibit the antiplatelet antibodies production by interfer...
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PMID: 19418731
PDF is available here.
Abstract
Glycoconjugates can be readily formed by the condensation of a free-reducing terminus and a strong alpha-effect nucleophile, such as a hydrazide or a hydroxylamine. Further characterization of a series of glycoconjugates formed from xylose, glucose and N-acetylglucosamine, and either p-toluenesulfon...
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PMID: 19056080
PDF is available here.