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Benzylidene Compounds (3):
Recent article
Benzylidene Compounds
Abstract
A series of (E)-2-(2-substituted benzylidene)- and 2-(2-substituted benzyl)-6-methoxy-tetralones were prepared, using an efficient synthetic scheme, and evaluated for their inhibitory activity against cytochrome P450C24A1 (CYP24A1) hydroxylase. In general the reduced benzyl tetralones were more acti...
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PMID: 20655626
PDF is available here.
PDF is available here.
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Abstract
4-Hydroxyphenylmethylene hydantoin (PMH, 1), isolated from the Red Sea sponge Hemimycale arabica, and delta-tocotrienol (3), isolated from the tocotrienol-rich fraction of palm oil, are important antimetastatic and antiproliferative natural products that proved effective against metastatic prostate...
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PMID: 21121261
PDF is available here.
PDF is available here.
Carbohydrate Research (345)13 2010
Abstract
Protecting groups often have profound influences on the stereoselectivity of glycosylation reactions. The effects of many protecting groups, especially cyclic protecting groups, are not well understood and difficult to explain and predict. Computational methods were used to study the effect of benzy...
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PMID: 20615497
PDF is available here.
PDF is available here.
Abstract
We have previously shown that achiral ferrocenyl diphenol butene derivatives are strong antitumor agents against both hormone-dependent and -independent breast cancer cell lines. We report now examples of a new series of two planar chiral diphenol derivatives, namely 1,2-[1-[1,1-bis(4-hydroxyphenyl)...
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PMID: 20614088
PDF is available here.
PDF is available here.
Abstract
I inhibitory activity.
Copyright (c) 2010 Elsevier Masson SAS. All rights reserved....
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PMID: 20202723
PDF is available here.
PDF is available here.
Chemical Communications (46)16 2010
Abstract
Two GFP analogues o-HBDI and o-HBMO have been designed and synthesized. The former shows no fluorescence while the latter shows strong fluorescence due to the formation of an intramolecular hydrogen-bond. At low temperatures, both molecules have strong fluorescence.
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PMID: 20369209
PDF is available here.
PDF is available here.
Abstract
Methacrylate resin-based sealers have attracted wide attention because of their easy handling, superior aesthetic qualities, good mechanical properties and excellent adhesive ability with dentin. 2,2-Bis[4-(2'-hydroxy-3'-methacryloyloxypropoxy)-phenyl]-propane (Bis-GMA) is the main component of the...
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PMID: 20507715
PDF is available here.
PDF is available here.
Alpha7 cholinergic-agonist prevents systemic inflammation and improves survival during resuscitation
Abstract
We report that the alpha7nAChR-agonist, GTS, restrains systemic inflammation and improves survival during resuscitation. Resuscitation with GTS rescued all the animals from lethal haemorrhage in a concentration-dependent manner. Unlike conventional resuscitation fluids, GTS inhibited the production...
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PMID: 19602049
PDF is available here.
PDF is available here.
Abstract
We describe the utility of this technology in the discovery of selective alpha7 agonists and PAMs. With alpha7 agonists, POETs experiments involved both single- and multiple-point concentration-response testing revealing diverse activation profiles (zero efficacy desensitizing, partial, and full ago...
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PMID: 19689206
PDF is available here.
PDF is available here.
Abstract
These results provide useful information to guide the development of new synthetic compounds for the treatment of allergic and inflammatory diseases related to histamine or mast cells....
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PMID: 19420752
PDF is available here.
PDF is available here.
Molecular Medicine (15)7-8 2009
Abstract
We report here our findings that GTS-21 attenuates tumor necrosis factor (TNF) and interleukin 1beta levels in human whole blood activated by exposure to endotoxin. GTS-21 inhibited TNF production in endotoxin-stimulated primary human monocytes in vitro at the transcriptional level. The suppressive...
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PMID: 19593403
PDF is available here.
PDF is available here.
Abstract
3-Substituted benzylidene-1,3-dihydro-indoline derivatives were tested for their in vitro antibacterial activity against the Gram-negative bacteria Klebsiella pneumoniae, Pseudomonas aeruginosa, Escherichia coli, and the Gram-positive bacteria Bacillus subtilis, Staphylococcus aureus, and for their...
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PMID: 19526705
PDF is available here.
PDF is available here.
Carbohydrate Research (344)1 2009
Abstract
H(2)SO(4)-silica-promoted removal of benzylidene, isopropylidene, trityl and tert-butyldimethylsilyl groups from sugar derivatives was accomplished by following an 'on-column' protocol in a virtually waste-free condition.
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PMID: 18977476
PDF is available here.
PDF is available here.
Abstract
We investigated expression of nicotinic acetylcholine receptors (nAChRs) in mucosal-type mast cells and their contribution to the regulation of mast cell activation. Expression of mRNA of nAChR alpha4, alpha7, and beta2 subunits were detected in specially differentiated mucosal-type murine bone marr...
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PMID: 18848921
PDF is available here.
PDF is available here.
Abstract
Assembly of the novel homochiral ligand L(S) (where L(S) is 1,4-benzylidene-bis(S,S)-4-yl-3,5-bis(1-hydroxyethyl)-1,2,4-triazole) and AgNO3 generates a robust, porous, chiral and cationic framework that exhibits reversible guest adsorption.
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PMID: 18985238
PDF is available here.
PDF is available here.
Organic Letters (10)21 2008
Abstract
2,3-Di-O-benzyl-4,6-O-benzylidene-thiohexopyranosides, on activation with 1-benzenesulfinyl piperidine and triflic anhydride, react with allyl silanes and stannanes, and with silyl enolethers to give C-glycosides. In the mannose series the beta-isomers are formed selectively whereas the glucose seri...
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PMID: 18826233
PDF is available here.
PDF is available here.
Abstract
We recently found that the anti-inflammatory potencies (suppression of iNOS and COX-2 expression) of a series of triterpenoids with Michael reaction centers were closely correlated with the potencies of these agents to induce the phase 2 response. We now report that representatives of seven recogniz...
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PMID: 18838692
PDF is available here.
PDF is available here.
Abstract
Compounds, in nanomolar to micromolar concentrations, exhibited growth inhibition and cytotoxicity in MCF-7 (breast) and HCT-116 (colon) cancer cells. In the NCI screen, 3,19-(2-bromobenzylidene) andrographolide (SRJ09) and 3,19-(3-chloro-4-fluorobenzylidene) andrographolide (SRJ23) showed greater...
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PMID: 18806812
PDF is available here.
PDF is available here.
Molecular Pharmacology (74)3 2008
Abstract
We report a mechanism by which EF24 potently suppresses the NF-kappaB signaling pathway through direct action on IkappaB kinase (IKK). We demonstrate that 1) EF24 induces death of lung, breast, ovarian, and cervical cancer cells, with a potency about 10 times higher than that of curcumin; 2) EF24 ra...
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PMID: 18577686
PDF is available here.
PDF is available here.
Abstract
A series of novel derivatives of the nonsteroidal anti-inflammatory drug (NSAID) sulindac sulfide were synthesized as potential agonists of the peroxisome proliferator-activated receptor gamma (PPARgamma). Nonpolar and aromatic substitutions on the benzylidene ring as well as retention of the carbox...
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PMID: 18665581
PDF is available here.
PDF is available here.
Abstract
Three series of structurally isomeric 2-benzylidene-6-(nitrobenzylidene) cyclohexanones 1-3 were prepared and evaluated against human Molt/C8 and CEM T-lymphocytes as well as murine L1210 cells. The IC(50) values of the majority of compounds are less than 10microM and in some assays, the figures for...
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PMID: 18450457
PDF is available here.
PDF is available here.
European Journal of Pharmacology (586)1-3 2008
Abstract
Opioid and excitatory amino acid receptors contribute to morphine dependence, but there are no studies of their role in heroin dependence. Thus, mice injected with acute or chronic heroin doses in the present study were pretreated with one of the following selective antagonists: 7-benzylidenenaltrex...
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PMID: 18343363
PDF is available here.
PDF is available here.
Endocrinology (149)5 2008
Abstract
We have examined the activity of a novel glucocorticoid receptor ligand that binds the receptor efficiently and strongly represses inflammatory gene expression. This compound has potent antiinflammatory activity in vivo and represses the transcription of the inflammatory cytokine monocyte chemoattra...
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PMID: 18218700
PDF is available here.
PDF is available here.
Abstract
We developed a method for selectively delivering EF24, a potent synthetic curcumin analog, to TF-expressing tumor vasculature and tumors using fVIIa as a drug carrier. EF24 was chemically conjugated to fVIIa through a tripeptide-chloromethyl ketone. After binding to TF-expressing targets by fVIIa, E...
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PMID: 18365880
PDF is available here.
PDF is available here.
Neuropeptides (42)2 2008
Abstract
We investigated the involvement of specific types of opioid receptors in methionine-enkephalin (MET)-induced modulation of hydrogen peroxide (H2O2) release by rat macrophages primed with sub-optimal concentrations of phorbol myristate acetate (PMA). Peritoneal macrophages in vitro treated with diffe...
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PMID: 18237778
PDF is available here.
PDF is available here.
Abstract
2-Heteroarylimino-5-benzylidene-4-thiazolidinones, unsubstituted or carrying hydroxy, methoxy, nitro and chloro groups on the benzene ring, were synthesised and assayed in vitro for their antimicrobial activity against gram positive and gram negative bacteria, yeasts and mould. The antimicrobial act...
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PMID: 18299196
PDF is available here.
PDF is available here.
Cancer Research (68)6 2008
Abstract
We assessed the in vivo therapeutic effects of EF24 on colon cancer cells. Using hexosaminidase assay, we determined that EF24 inhibits proliferation of HCT-116 and HT-29 colon and AGS gastric adenocarcinoma cells but not of mouse embryo fibroblasts. Furthermore, the cancer cells showed increased le...
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PMID: 18339878
PDF is available here.
PDF is available here.
Abstract
I and S spins and has been named as EXE-MS2. The proposed scheme which has a scaling factor of 1 is observed to be free from low intensity artifacts and provides better line-widths particularly for S spins labeled at multiple sites. The pulse sequence which has been applied on static oriented sample...
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PMID: 18406111
PDF is available here.
PDF is available here.
Abstract
Two series of 4-benzylideneamino- and 4-phenyliminomethyl-benzenesulfonamide derivatives were designed and synthesized for the evaluation as selective cyclooxygenase-2 (COX-2) inhibitors in a cellular assay using human whole blood (HWB). Extensive structure-activity relationships (SAR) were studied...
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PMID: 18063374
PDF is available here.
PDF is available here.
Abstract
Abstract
A series of 3,5-bis(benzylidene)piperidin-4-ones 1, 1-acryloyl-3,5-bis(benzylidene)piperidin-4-ones 2 and adducts of 2 with sodium 2-mercaptoethanesulfonate (mesna), namely series 3, were prepared as candidate cytotoxic agents. These compounds were examined against neoplastic HSC-2, HSC-4 and HL-60...
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PMID: 17499885
PDF is available here.
PDF is available here.
Anticancer Research (28)5A 2008
Abstract
The cytotoxic activity of sodium 5,6-benzylidene-L-ascorbate (SBA) against eight human cancer cell lines and three human normal cells was investigated, SBA showed slightly higher cytotoxicity against human tumor cell lines, as compared with normal cells, with a tumor-specificity index of 2.0. The hu...
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PMID: 19035281
PDF is available here.
PDF is available here.
Abstract
A series of Schiff bases including N-benzylideneaniline (NBA) nuclei were prepared. The chemical products obtained were characterized by mass spectometry (APCI), 1H NMR, and IR spectroscopy in order to seek their cytotoxic and proliferation effects on human small lung (A549) and cervical (HeLa) canc...
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PMID: 17457959
PDF is available here.
PDF is available here.
Abstract
A series of 3-benzylidene-7-alkoxychroman-4-one derivatives were synthesized and evaluated for their antioxidant activities. The antioxidant activity was assessed using three methods, namely, 1,1-diphenyl-2-picrylhydrazyl (DPPH) radical scavenging, ferric reducing antioxidant power (FRAP), and thiob...
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PMID: 17967537
PDF is available here.
PDF is available here.
Abstract
We have developed a series of glucocorticoid receptor (GR) ligands that retain the strong antiinflammatory activity of conventional glucocorticoids with reduced side effects. We present a compound, LGD5552, that binds the receptor efficiently and strongly represses inflammatory gene expression. LGD5...
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PMID: 18032610
PDF is available here.
PDF is available here.
Abstract
The cholinergic nervous system can inhibit the release of proinflammatory cytokines such as TNF-alpha from LPS-stimulated macrophages. Acetylcholine, the principal neurotransmitter of the vagus nerve, is the key mediator of this so-called cholinergic anti-inflammatory pathway, specifically interacti...
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PMID: 17621262
PDF is available here.
PDF is available here.
Abstract
The crystal structures of 9-[(E)-2-(4-fluorophenyl)vinyl]-9H-carbazole, C20H14FN, (I), 9-[(E)-2-(4-chlorophenyl)vinyl]-9H-carbazole, C20H14ClN, (II), and 9-[(E)-2-(4-bromophenyl)vinyl]-9H-carbazole, C20H14BrN, (III), are determined mainly by van der Waals forces. The chloro and bromo derivatives are...
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PMID: 18057632
PDF is available here.
PDF is available here.
European Journal of Pharmacology (575)1-3 2007
Abstract
We examined the effect of the molecules on cell cycle progression, organization of microtubule networks, and apoptosis induction. As determined by flow cytometry, cancer cells were predominantly arrested in metaphase with 4N DNA before cell death occurred. By using indirect immunofluorescence techni...
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PMID: 17707367
PDF is available here.
PDF is available here.
Abstract
The birefringence of MBBA, determined from the channeled spectra, decreases when the wavelength increases, showing a normal dispersion. The changes induced by an external electrostatic field acting perpendicular on the nematic director in the birefringence values were evidenced. The birefringence in...
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PMID: 17306616
PDF is available here.
PDF is available here.
Biochemical Pharmacology (74)8 2007
Abstract
Current antipsychotic treatments fail to fully address the range of symptoms of schizophrenia, particularly with respect to social and occupational dysfunctions. Recent work has highlighted the role of nicotinie in both cognitive and attentional deficits as well as deficient processing of repetitive...
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PMID: 17714692
PDF is available here.
PDF is available here.
Carbohydrate Research (342)14 2007
Abstract
The first total synthesis of a novel alpha-galactoglycosphingolipid clarhamnoside has been achieved through a straightforward strategy. A thiogalactosyl donor with a benzylidene group at C-4 and C-6 and nonparticipating p-methoxybenzyl group at C-2 was successfully employed in the stereocontrolled s...
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PMID: 17559820
PDF is available here.
PDF is available here.
Abstract
A series of 6-mono-, di-, and trifluoro analogs of S-phenyl 2,3,4-tri-O-benzyl-D- or L-thiorhamnopyranoside has been synthesized and used as donors in glycosylation reactions, with activation by the 1-benzenesulfinyl piperidine/triflic anhydride system. The stereochemical outcome of the glycosylatio...
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PMID: 17725351
PDF is available here.
PDF is available here.
Journal of Biological Chemistry (282)39 2007
Abstract
Our results clearly suggested that EF24 induced significant increase in PTEN expression. The up-regulation of PTEN inhibited Akt and MDM2, which enhanced the level of p53, thereby inducing G(2)/M arrest and apoptosis. Therefore, EF24 appears to have a potential therapeutic role in human ovarian canc...
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PMID: 17684018
PDF is available here.
PDF is available here.
Abstract
A novel series of aurone derivatives for in vivo imaging of beta-amyloid plaques in the brain of Alzheimer's disease (AD) were synthesized and characterized. When in vitro binding studies using Abeta(1-42) aggregates were carried out with aurone derivatives, they showed high binding affinities for A...
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PMID: 17644062
PDF is available here.
PDF is available here.
Abstract
In the title potential O,N,N',O'-tetradentate Schiff base ligand {systematic name: 2,2'-[pentane-1,5-diylbis(nitrilomethylidyne)]diphenol}, C(19)H(22)N(2)O(2), the mutual orientation of the three planar fragments determines the conformation of the molecule. The dihedral angles between the planes of...
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PMID: 17762133
PDF is available here.
PDF is available here.
Molecular Pharmacology (72)3 2007
Abstract
We investigated interactions of these compounds at human alpha7 nAChRs, expressed in Xenopus laevis oocytes, along with genistein, a tyrosine kinase inhibitor. Genistein was found to function as a PAM. Two types of PAM profiles were observed. 5-HI and genistein predominantly affected the apparent pe...
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PMID: 17565004
PDF is available here.
PDF is available here.
Abstract
Raman and FTIR spectra of 2-phenyl-4-(4-methoxy benzylidene)-2-oxazolin-5-one were recorded in the regions, 100-3300 and 400-4000 cm(-1), respectively. Vibrational frequencies and intensities of the fundamental modes of this hetrocyclic organic molecule were computed using ab initio as well as AM1 s...
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PMID: 17045517
PDF is available here.
PDF is available here.
Abstract
In the title compound, C(9)H(12)N(5)O(3)(+) x Cl(-), the cation is almost entirely planar. The imine double bond is exclusively in the E geometry.
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PMID: 17609569
PDF is available here.
PDF is available here.
Abstract
The major findings are as follows: (a) extremely rapid uptake and clearance of [2-methoxy-(11)C]GTS-21 from the brain, which may need to be considered in developing optimal dosing of GTS-21 for patients, and (b) significant brain uptake of 2-OH-GTS-21, suggesting that it might contribute to the ther...
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PMID: 17591554
PDF is available here.
PDF is available here.
Abstract
We have investigated the selectivity of pharmacologically selective delta and kappa antagonists in mice by both i.t. and i.c.v. routes of administration to evaluate changes in selectivity. Using pharmacologically selective delta (benzylidenenaltrexone, naltrindole, and naltriben) and kappa (norbinal...
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PMID: 17400888
PDF is available here.
PDF is available here.
Abstract
Langmuir and Langmuir-Blodgett monolayers of N-(4-octadecyloxy-2-hydroxybenzylidene) derivatives of glycine, tyrosine, and phenylalanine were studied using pi-A isotherms and photoelastic modulated FTIR (PEM-FTIR). Based on compression modulus and interaction parameters, mixed monola...
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PMID: 17306822
PDF is available here.
PDF is available here.
Abstract
We present the discovery of a rhodanine (2-thioxothiazolidin-4-one) class of compounds as inhibitors of this enzyme using a combined approach of rational selection of compounds for screening, analogue search, docking studies, and lead optimization. The most potent inhibitor exhibits an IC(50) of 35....
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PMID: 17477517
PDF is available here.
PDF is available here.
Abstract
These results demonstrate that antagonist efficacy is context-dependent, possibly accounting for paradoxical pharmacological effects. Activity profiles at the three opioid receptors under different conditions could lead to antagonists with optimal clinical properties in treatment of addiction and ad...
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PMID: 17267582
PDF is available here.
PDF is available here.
Abstract
Cinnamoly compounds 1a-c and 2a-d were designed, synthesized, and in vitro tested as p300 inhibitors. At different degrees, all tested compounds were proven to inactivate p300, particularly, derivative 2c was the most active inhibitor, also showing high specificity for p300 as compared to other hist...
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PMID: 17348637
PDF is available here.
PDF is available here.
Abstract
We here investigated the capacity of the selective alpha7 cholinergic receptor agonist 3-(2,4-dimethoxybenzylidene) anabaseine (GTS-21) to inhibit LPS-induced inflammatory responses in mice in vivo. To this end, mice received an intraperitoneal injection of LPS (from Escherichia coli, 200 microg) pr...
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PMID: 17414429
PDF is available here.
PDF is available here.
Critical Care Medicine (35)4 2007
Abstract
Critical Care Medicine (35)4 2007
Abstract
GTS-21 dose-dependently inhibited tumor necrosis factor and high mobility group box 1 release and nuclear factor-kappaB activation in vitro. GTS-21 (4 mg/kg) significantly inhibited serum tumor necrosis factor during endotoxemia and improved survival (p < .0001). GTS-21 (4 mg/kg) significantly inhib...
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PMID: 17334244
PDF is available here.
PDF is available here.
Abstract
Human protein kinase CK2 is an ubiquitous serine/threonine kinase that is typically found in tetrameric complexes consisting of two catalytic (alpha and/or alpha') and two regulatory beta subunits. Although there is growing evidence that besides the participation of CK2 in a complex series of cellul...
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PMID: 17409508
PDF is available here.
PDF is available here.
Neuroscience (145)1 2007
Abstract
Brain alpha7 nicotinic receptors have become therapeutic targets for Alzheimer's disease (AD) based on their memory-enhancing and neuroprotective actions. This study investigated the feasibility of increasing neuronal alpha7 receptor functions using a gene delivery approach based on neuron-selective...
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PMID: 17218065
PDF is available here.
PDF is available here.
Carbohydrate Research (342)3-4 2007
Abstract
Methanesulfonic acid was shown to be an efficient and convenient substitute for ethereal HCl in reductive 4,6-O-benzylidene acetal ring-opening reaction with sodium cyanoborohydride in THF. Normal regioselectivity was observed, the 6-O-benzyl ethers with free 4-OH group being the major products of t...
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PMID: 17118348
PDF is available here.
PDF is available here.