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Heterocyclic Compounds with 4 or More Rings (13):
Recent article
Heterocyclic Compounds with 4 or More Rings
Organic Letters (13)14 2011
Abstract
A copper-catalyzed aerobic oxidative intramolecular alkene C-H amination has been developed using readily available substituted 3-benzylidene-2-pyridin-2-ylmethyl-2,3-dihydro-isoindol-1-ones as the starting materials, and the corresponding N-heterocycles were obtained in good to exce...
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PMID: 21696194
PDF is available here.
PDF is available here.
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Abstract
We predict that the true structure of nobilisitine A is likely the diastereomer shown here or its enantiomer....
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PMID: 21469691
PDF is available here.
PDF is available here.
Abstract
We present a novel pharmacological approach that targets inflammatory gene expression by interfering with the recognition of acetylated histones by the bromodomain and extra terminal domain (BET) family of proteins. We describe a synthetic compound (I-BET) that by 'mimicking' acetylated histones dis...
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PMID: 21068722
PDF is available here.
PDF is available here.
Behavioural Brain Research (214)2 2010
Abstract
Deficits in reversal learning induced by acute d-amphetamine were attenuated by risperidone (0.2mg/kg i.p.). Acute PCP-induced impairment of reversal learning was attenuated by acute asenapine (0.025 mg/kg subcutaneously [s.c.]), risperidone (0.2mg/kg i.p.), and olanzapine (1.0mg/kg i.p.). Subchroni...
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PMID: 20561963
PDF is available here.
PDF is available here.
Abstract
A new family of pentacyclic compounds incorporating a central 1,2-dihydropyridine core is obtained through a pseudo three-component reaction. Four new bonds and two stereocenters with trans relationship are produced during the cascade process under palladium catalysis.
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PMID: 20844800
PDF is available here.
PDF is available here.
Abstract
We treated primary erythroblasts with inhibitors of cytokinesis, including blebbistatin, hesperadin, and nocodazole, and then assayed for enucleation. Although these agents inhibited cell-cycle progression and subsequent enucleation when added early in culture, they failed to block enucleation prope...
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PMID: 20644112
PDF is available here.
PDF is available here.
FASEB Journal (24)11 2010
Abstract
We investigated the regulation of Cx43-hemichannel activity by actomyosin contractility and intracellular [Ca(2+)] ([Ca(2+)](i)) using plasma membrane-permeable TAT peptides (100 μM) designed to interfere with interactions between the cytoplasmic loop (CL) and carboxy-terminal (CT) in primary bovin...
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PMID: 20634352
PDF is available here.
PDF is available here.
Fitoterapia (81)6 2010
Abstract
Although the quinolizidine alkaloids and flavonoids, the main active components of the traditional Chinese medicine Sophora flavescens, have been largely investigated, a new matrine alkaloid derivative 9alpha-hydroxy-7,11-dehydromatrine (1) and a rare 1,4-diazaindan-type alkaloid flavascensine (17),...
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PMID: 20079811
PDF is available here.
PDF is available here.
Thrombosis and Haemostasis (104)2 2010
Abstract
We evaluated the enzyme kinetics, antithrombotic and antihaemostatic properties of BMS-593214, an active-site, direct FVIIa inhibitor. Studies were conducted in enzymatic assays, and in anesthetised rabbit models of electrically-induced carotid arterial thrombosis (AT), thread-induced vena cava veno...
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PMID: 20589312
PDF is available here.
PDF is available here.
Infection and Immunity (78)7 2010
Abstract
We previously demonstrated that efficient C. parvum invasion of biliary epithelial cells (cholangiocytes) requires host cell actin polymerization and localized membrane translocation/insertion of Na(+)/glucose cotransporter 1 (SGLT1) and of aquaporin 1 (Aqp1), a water channel, at the attachment site...
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PMID: 20457792
PDF is available here.
PDF is available here.
Advanced Materials (FRG) (22)25 2010
Abstract
Advanced Materials (FRG) (22)25 2010
Abstract
Abstract
We demonstrate that Lam D and structural analogues induce apoptosis of cancer cells by acting directly on mitochondria inducing reduction of mitochondrial membrane potential, swelling and cytochrome c release. Cyclosporin A, a well-known inhibitor of MPT, completely prevents mitochondrial signs of a...
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PMID: 20151196
PDF is available here.
PDF is available here.
Circulation (121)25 2010
Abstract
These results suggest that nonuniformity of muscle contraction is an important determinant of the sustainability and frequency of triggered arrhythmias caused by the surge of Ca(2+) dissociated from myofilaments in cardiac muscle....
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PMID: 20547931
PDF is available here.
PDF is available here.
Abstract
Eight pentacyclic compounds, xestosaprols F-M (1-8), were isolated from a marine sponge belonging to the genus Xestospongia. The structures of these new compounds were determined on the basis of extensive analyses of NMR experiments and mass spectrometric measurements. These compounds inhibited the...
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PMID: 20503979
PDF is available here.
PDF is available here.
Abstract
We have determined the experimental logP values of a set of 25 lamellarins, given it is the single most important parameter in determining multiple ADMET parameters. We also discuss the relationship between this natural product class, natural product derivatives in development and on the market, ora...
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PMID: 20167395
PDF is available here.
PDF is available here.
Chemical Communications (46)19 2010
Abstract
We report here two novel 2,7-fluorene- and 2,7-carbazole-based conjugated polymers PFDCTBT and PCDCTBT containing ladder-type heptacyclic structures with forced planarity. PCDTBT shows excellent solubility, low band gap and high hole mobility, leading to a power conversion efficiency of 3.7%.
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PMID: 20393657
PDF is available here.
PDF is available here.
Abstract
The total synthesis of the Lycopodium alkaloid complanadine A, which is an unsymmetrical dimer of lycodine, was achieved by exploiting a common tetracyclic precursor. Key to the success of the synthesis was the development of a late-stage site-selective C-H functionalization of a pyridine moiety to a...
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PMID: 20387895
PDF is available here.
PDF is available here.
Abstract
A total synthesis of the Lycopodium alkaloid (+)-complanadine A is described. Complanadine A has been shown to induce the secretion of neurotrophic factors from 1321N1 cells, promoting the differentiation of PC-12 cells. The use of a simplifying metal mediated [2+2+2] + [2+2+2] sequence using a sily...
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PMID: 20387896
PDF is available here.
PDF is available here.
Journal of Cell Science (123)Pt 9 2010
Abstract
We characterised podosomes of immature dendritic cells using electron microscopy combined with both conventional and novel high-resolution structured illumination light microscopy. Dendritic cell podosomes are composed of actin foci surrounded by a specialised ring region that is rich in material co...
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PMID: 20356925
PDF is available here.
PDF is available here.
Abstract
I disorder. Asenapine's in vitro profile is similar to other atypical antipsychotic agents insofar as there is higher affinity for serotonin 5-HT(2A) versus dopamine D(2) receptors. Asenapine exhibits a unique effect on monoamine, histamine and muscarinic receptor affinities, as well as effects on N...
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PMID: 20420486
PDF is available here.
PDF is available here.
Abstract
An oxidative cyclization of dienic sulfonamides mediated by iodobenzene diacetate in TFA, followed by a tandem intramolecular Diels-Alder reaction, achieves desymmetrization of a "locally symmetrical" dienone with good levels of diastereoselectivity and leads to valuable synthetic intermediates for...
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PMID: 20329732
PDF is available here.
PDF is available here.
Abstract
We established a chemical screen for small molecules that suppress steroid-inducible and RPM1-avrRpm1-dependent cell death in Arabidopsis seedlings. Screening of a library comprising 6,800 compounds of natural origin identified two trichothecene-type mycotoxins, 4,15-diacetoxyscirpenol (DAS) and neo...
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PMID: 20140739
PDF is available here.
PDF is available here.
Abstract
Preliminary pharmacological study was conducted for the pterocarpans macckian (Mac) and trifolirhizin (Trif). The two compounds isolated from Ononis vaginalis were tested for their hepatoprotective effects against CCl4 induced hepatotoxicity in rats. Activity was accessed by measuring liver enzymes...
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PMID: 20363697
PDF is available here.
PDF is available here.
Abstract
Purpose. To determine the role of actin cytoskeleton in the disassembly and reformation of adherens junctions (AJs) and tight junctions (TJs) in bovine corneal endothelial monolayers. Methods. Disassembly and reformation of AJs and TJs were induced by extracellular Ca(2+) depletion and subsequent ad...
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PMID: 20019371
PDF is available here.
PDF is available here.
Abstract
Adrenergic (alpha1 and alpha2) and cholinergic muscarinic (M1-M5) receptor binding in rat forebrain was quantified after 4 wk of twice-daily subcutaneous administration of asenapine or vehicle. Asenapine (0.03, 0.1, and 0.3 mg/kg) produced increases in [3H]prazosin binding to alpha1-adrenergic recep...
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PMID: 19835670
PDF is available here.
PDF is available here.
Chemical Communications (46)13 2010
Abstract
New functionalized ethano-bridged Tröger bases are readily prepared using a simple alkylation/rearrangement sequence which affords configurationally stable derivatives as single stereoisomers (de > 96%).
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PMID: 20234907
PDF is available here.
PDF is available here.
Abstract
Inhibition of acetylcholinesterase (AChE) and therefore prevention of acetylcholine degradation is one of the most accepted therapy opportunities for Alzheimer s disease (AD), today. Due to lack of selectivity of AChE inhibitor drugs on the market, AD-patients suffer from side effects like nausea or...
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PMID: 20176490
PDF is available here.
PDF is available here.
Abstract
We have studied the spatiotemporal pattern of blebbistatin-induced anomalous electrical activities in isolated rat atrial preparations using the optical mapping of excitation spread. Atrial preparations including the right or left auricle were dissected from adult rat hearts. Each preparation was th...
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PMID: 20013327
PDF is available here.
PDF is available here.
Abstract
We developed a novel atomic force microscope elastography technique for mapping spatiotemporal stiffness of isolated, spontaneously beating neonatal rat cardiomyocytes. Cells were indented repeatedly at a rate close but unequal to their contractile frequency. The resultant changes in pointwise appar...
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PMID: 20023124
PDF is available here.
PDF is available here.
Organic Letters (12)3 2010
Abstract
A highly efficient and concise synthetic scheme for rhodol fluorophores is developed with palladium-catalyzed amination reaction as the key step. This new synthetic route is utilized to construct a rhodol library, potentially useful for the design of novel fluorescent probes....
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PMID: 20067265
PDF is available here.
PDF is available here.
Journal of Cell Biology (188)2 2010
Abstract
We analyzed the relationship between actin network velocity and traction forces at the substrate in a model system of persistently migrating fish epidermal keratocytes. Front and lateral sides of the cell exhibited much stronger coupling between actin motion and traction forces than the trailing cel...
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PMID: 20100912
PDF is available here.
PDF is available here.
Tsitologiia (52)1 2010
Abstract
We studied their role during spreading of normal and transformed REF52tetRas fibroblasts with adjustable ras oncogene expression. Treatment with inhibitors of cell contractility (Y27532 or blebbistatin) led to disappearance of actin bundles and focal adhesions, but both normal and transformed cells...
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PMID: 20302016
PDF is available here.
PDF is available here.
Abstract
From the cultures of spore-derived mycobionts of the lichen Lecanora leprosa a novel naphtho[1,8-cd]pyran-3-one derivative, lecanopyrone, was isolated. Its structure was determined by spectroscopic methods. The assembly pattern of acetate units in its biosynthesis was verified using...
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PMID: 21319703
PDF is available here.
PDF is available here.
Abstract
Despite abolishing cardiac contractility, BDM altered ventricular AP morphology and inhibited spontaneous APs. In contrast, blebbistatin (10 microM) abolished contractility without significantly altering AP morphology or generation of spontaneous APs. Blebbistatin allowed for high fidelity measureme...
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PMID: 20332622
PDF is available here.
PDF is available here.
Abstract
I inhibition and a mitochondrial targeting. The present study was designed to investigate the contribution of these two pathways for apoptosis in cancer cells. Lamellarin D promoted nuclear apoptosis in leukemia cells without prominent cell cycle arrest. Signals transmitted by lamellarin D initiated...
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PMID: 19952118
PDF is available here.
PDF is available here.
Abstract
OBJECTIVE: To develop a Quantitative Assay of Multi-components by Single - marker (QAMS) for simultaneous determination of three components in Fructus Evodiae, and examine the feasibility of using the relative correction factors between the different types of compounds. METHOD: Rutaecarpine was sele...
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PMID: 20209915
PDF is available here.
PDF is available here.
Abstract
Carpanone has been stereoselectively synthesized in 55% yield and six steps from sesamol. The key step of the synthetic sequence is the direct introduction of the propenyl side chain via a Suzuki-Miyaura cross-coupling reaction. The subsequent Pd(II)-catalyzed oxidative coupling yields carpanone as...
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PMID: 19725522
PDF is available here.
PDF is available here.
Abstract
I disorder, sublingual asenapine produced significantly greater reductions from baseline than placebo in clinician-assessed Young Mania Rating Scale (YMRS) total score at 3 weeks. In two randomized, controlled trials in adult patients with acute schizophrenia, treatment with asenapine reduced from b...
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PMID: 19689168
PDF is available here.
PDF is available here.
Biochemistry (Washington) (48)33 2009
Abstract
We investigated the binding of two halichondrin B analogues, eribulin (previously, ER-086526, E7389) and ER-076349, to tubulin by quantitative analytical ultracentrifugation. Eribulin is currently undergoing phase III clinical trials for cancer; ER-076349 is a closely related analogue with C.35 hydr...
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PMID: 19586046
PDF is available here.
PDF is available here.
Abstract
A synthesis providing totally synthetic (+)-hemi-phorboxazole A (1), proceeding in two steps (85% yield) from known vinyl iodide precursor (+)-2, has been achieved in conjunction with the design, synthesis, and biological evaluation of two hemi-phorboxazole analogues [(+)-3 and (-)-4] featuring ring...
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PMID: 19637861
PDF is available here.
PDF is available here.
Inorganic Chemistry (48)15 2009
Abstract
Multifrequency electron paramagnetic resonance (EPR) spectroscopy is used to explore the electronic structures of a series of dicopper complexes of the type {(LXL)Cu}(2)(+). These complexes contain two four-coordinate copper centers of highly distorted tetrahedral geometries linked by two [LXL](-) l...
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PMID: 19572723
PDF is available here.
PDF is available here.
Abstract
We describe the first total synthesis of (-)-himandrine, a member of the class II galbulimima alkaloids. Noteworthy features of this chemistry include a diastereoselective Diels-Alder reaction in the rapid synthesis of the tricycle ABC-ring system in an enantiomerically enriched form, the use of a f...
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PMID: 19555115
PDF is available here.
PDF is available here.
Abstract
A total synthesis of the complex, bent aromatic ring-containing marine alkaloid haouamine A is achieved through a route in which every step (with the exception of the final deprotection) is performed on a gram-scale. This is accomplished through the development of a method for the dehydrogenation of...
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PMID: 19530671
PDF is available here.
PDF is available here.
FEBS Letters (583)12 2009
Abstract
We analyzed the apoptotic effect of SNX-2112 on human chronic myeloid leukemia (CML) K562 cells. Transcriptomic and proteomic approaches further revealed that caspase signals originated from mitochondria dysfunction, mediated by Akt signaling pathway inactivity. Additionally, SNX-2112 prolonged the...
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PMID: 19427857
PDF is available here.
PDF is available here.
Abstract
Heterotrimeric G protein signaling regulates many processes in fungi, such as development, pathogenicity, and secondary metabolite biosynthesis. For example, the Galpha subunit Pga1 from Penicillium chrysogenum regulates conidiation and secondary metabolite production in this fungus. The dominant ac...
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PMID: 19784932
PDF is available here.
PDF is available here.
Abstract
Three known compounds, stemofoline (1), (2'S)-hydroxystemofoline (2), and (11Z)-1',2'-didehydrostemofoline (3), along with two new alkaloids, stemaphylline (4) and stemaphylline-N-oxide (5), have been isolated from a root extract of Stemona aphylla. The structures of these alkaloids were determined...
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PMID: 19374387
PDF is available here.
PDF is available here.
Biophysical Journal (96)9 2009
Abstract
We showed that there was a close correlation between the conformation of the myosin heads on the surface of the thick filaments and the extent of their helical order. Helical order required the heads to be in the closed conformation. In addition, we showed that, with the same ligand bound at the act...
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PMID: 19413972
PDF is available here.
PDF is available here.
Organic Letters (11)7 2009
Abstract
An unexpected rearrangement of haemanthamine-type alkaloids in the presence of halogenating agents has been found. Rearranged compounds present the 5,11-methanomorphantridine framework characteristic of montanine-type alkaloids. These compounds are difficult to obtain because of thei...
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PMID: 19320502
PDF is available here.
PDF is available here.
Abstract
A new domino reaction for the highly selective synthesis of tetracyclic cinnolino[5,4,3-cde]cinnolines using steric control was described. In this reaction, the use of anthenes with aliphatic groups (R(1)) leads to cinnolino[5,4,3-cde]cinnolines whereas anthenes with aryl groups (R(1)) result in N-a...
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PMID: 19262937
PDF is available here.
PDF is available here.
Organic Letters (11)5 2009
Abstract
A novel and general halopalladation/decarboxylation/carbon-carbon forming domino protocol is described for the synthesis of 5-halo-6-substituted benzo[b]naphtho[2,1-d]furans. The protocol represents the first example of trapping the sigma-vinylpalladium intermediate, generated from h...
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PMID: 19199490
PDF is available here.
PDF is available here.
Protein Science (18)3 2009
Abstract
We cloned the entire sequence of mouse SIRT3, as well as rat and rabbit SIRT3. Importantly, we find that full-length SIRT3 protein localizes exclusively to the mitochondria, in contrast to reports of SIRT3 localization to the nucleus. We demonstrate that SIRT3 has no deacetylation activity in vitro...
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PMID: 19241369
PDF is available here.
PDF is available here.
Abstract
An alpha-hydroxyaldehyde derived from naltrexone was converted to an oxazoline dimer with ammonium chloride and sodium acetate in MeOH under reflux. The resulting dimer was treated with dl-camphorsulfonic acid in CHCl(3) to give the trimer. The method for trimer synthesis was also ap...
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PMID: 19115979
PDF is available here.
PDF is available here.
Abstract
A new chiral molecular tweezer was synthesized with (1R,2R)-1,2-diaminocyclohexane as spacer and two molecules of (+)-usnic acid as pincers. The ability of this molecular tweezer to bind 2,4,7-trinitrofluorenone was studied. A charge-transfer complex was formed in which TNF was sandw...
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PMID: 19125581
PDF is available here.
PDF is available here.
Abstract
A tandem ketene-trapping/Diels-Alder cyclization sequence was the pivotal transformation in an efficient, asymmetric synthesis of a decahydrofluorene tricyclic structure possessing eight stereogenic centers and key features of the hirsutellone class of antitubercular natural products...
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PMID: 19119873
PDF is available here.
PDF is available here.
Abstract
A novel type of hemispherical cage was synthesized in a one-pot procedure, which displayed good binding properties towards nickel(ii).
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PMID: 19209323
PDF is available here.
PDF is available here.
Abstract
trans-4-Hydroxy-L-proline was converted into a tricyclic compound representing three contiguous rings of the anticancer antibiotic MPC1001. The tricyclic model contains the dihydrooxepin and diketopiperazine subunits, as well as one of the sulfur atoms of the natural product. The diketopiperazine un...
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PMID: 19067592
PDF is available here.
PDF is available here.
Biophysical Journal (96)2 2009
Abstract
We have investigated the role of cell-derived traction forces in the assembly of extracellular matrix using what we believe is a novel assay that allows for simultaneous measurement of traction forces and fibronectin fibril growth at discrete cell-matrix attachment sites. NIH3T3 cells were plated on...
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PMID: 19167317
PDF is available here.
PDF is available here.
Abstract
Antioxidant agents against reactive oxygen species can be used for several cosmetic and medicinal applications. This study's objective was to evaluate the antioxidant activities of Polytrichastrum alpinum (Hedw.) G. L. Sm. (Polytrichaceae), an Antarctic moss species collected from King George Island...
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PMID: 19526712
PDF is available here.
PDF is available here.
Oncology Research (18)5-6 2009
Abstract
We report on a novel small molecule inhibitor of Hsp90, SNX-2112, and an orally bioavailable prodrug analog, SNX-5422. In cellular models of wild-type or mutant EGFR (L858R and T790M mutations), SNX-2112 alone and in combination with erlotinib inhibited EGF activation of pAKT(473) and pSTAT3(705). p...
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PMID: 20225761
PDF is available here.
PDF is available here.