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Heterocyclic Compounds, 3-Ring (20):
Recent article
Heterocyclic Compounds, 3-Ring
Abstract
Inhibitors of B-Raf and MEK kinases hold promise for the management of cutaneous melanomas harboring BRAF mutations. BRAF mutations are rare in uveal melanomas (UMs), but somatic mutations in the G protein α subunits Gαq and Gα11 (encoded by GNAQ and GNA11, respectively) occur in...
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PMID: 21828154
PDF is available here.
PDF is available here.
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Abstract
Abstract
We wanted to investigate possible routes via ring opening of alpha-amino phosphonates with an oxanorbornene skeleton, as these can be synthesized with high stereoselectivity. This was achieved using different Lewis acids, leading to a range of products. The reaction with TiCl(4) and FeCl(3) was mode...
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PMID: 20544085
PDF is available here.
PDF is available here.
Abstract
We evaluated the effect of a novel allosteric Akt inhibitor, MK-2206, in combination with several anticancer agents. In vitro, MK-2206 synergistically inhibited cell proliferation of human cancer cell lines in combination with molecular targeted agents such as erlotinib (an epidermal growth factor r...
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PMID: 20571069
PDF is available here.
PDF is available here.
Abstract
We addressed this hypothesis by perturbing the inflammatory milieu of the hypothalamus in adult male Wistar rats using intracerebroventricular (icv) administration of interleukin-4 (IL-4), a Th2 cytokine that promotes alternative activation (M2) of macrophages and microglia. During HF feeding, icv I...
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PMID: 20371733
PDF is available here.
PDF is available here.
Abstract
We have developed a simple and straightforward procedure for the enantioselective preparation of densely substituted bicyclic and tricyclic nitrogen heterocycles using conveniently substituted enantiopure pyrrolidines as common synthetic intermediates, which are easily accessible by our recently dev...
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PMID: 20401401
PDF is available here.
PDF is available here.
Abstract
TMC435 is a small-molecule inhibitor of the NS3/4A serine protease of hepatitis C virus (HCV) currently in phase 2 development. The in vitro resistance profile of TMC435 was characterized by selection experiments with HCV genotype 1 replicon cells and the genotype 2a JFH-1 system. In 80% (86/109) of...
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PMID: 20176898
PDF is available here.
PDF is available here.
Abstract
In this study, potential inhibitory effect of 21 species of marine algae on melanogenesis was assessed via tyrosinase inhibitory effect. The Ishige okamurae extract tested herein evidenced profound tyrosinase inhibitory effect, compared to that exhibited by other marine algae extracts. Thus, I. okam...
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PMID: 20211676
PDF is available here.
PDF is available here.
Abstract
I clinical trials for the treatment of advanced solid tumors. In intact cells, the inhibitory activity of PF-03814735 on the Aurora1 and Aurora2 kinases reduces levels of phospho-Aurora1, phosphohistone H3, and phospho-Aurora2. PF-03814735 produces a block in cytokinesis, resulting in inhibition of...
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PMID: 20354118
PDF is available here.
PDF is available here.
Abstract
The fifth international conference on SUMO, Ubiquitin, UBL Proteins: Implications for Human Diseases, held in Houston, included topics covering the latest advances and new targets in the field of protein modification. This conference report highlights selected presentations on the structural charact...
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PMID: 20373248
PDF is available here.
PDF is available here.
Planta Medica (76)3 2010
Abstract
A phenylpropanoid 1, a slovenolide 2, and two germacranes bearing a methylthiopropenoate moiety, 3 and 4, along with twenty known metabolites have been isolated from the roots of Thapsia villosa var. villosa L. The structures of two known phenylpropanoids 5 and 6 have been corrected. Compounds 7 and...
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PMID: 19708003
PDF is available here.
PDF is available here.
Abstract
These results suggest that in the rat mesenteric artery, cassiarin A-induced relaxation may be mediated by endothelial NO and may occur partly via BK(Ca)-channel activation....
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PMID: 20460764
PDF is available here.
PDF is available here.
Abstract
A new metabolite, 7-hydroxyjanthinone (1), was isolated from the mangrove endophytic fungus Penicillium sp. (SBE-8), together with two known compounds, janthinone (2) and citrinin (3). The structures of these compounds were identified by spectroscopic methods. Compounds 1 and 2 showed no cytotoxicit...
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PMID: 19967978
PDF is available here.
PDF is available here.
Journal of Antibiotics (62)9 2009
Abstract
Journal of Physical Chemistry A: Molecules, Spectroscopy, Kinetics, Environment and General Theory (113)33 2009
Abstract
With 4-fluorofluorazene (FPP4F) and its flexible counterpart 4-fluoro-N-phenylpyrrole (PP4F) an intramolecular charge transfer (ICT) reaction occurs in the singlet excited state in sufficiently polar solvents. The ICT reaction begins to appear in tetrahydrofuran (epsilon = 7.4) for FPP4F and in the...
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PMID: 19719292
PDF is available here.
PDF is available here.
Organic Letters (11)15 2009
Abstract
The synthesis of prodrugs targeted to the SH2 domain of Stat3 is reported. Using a convergent strategy, the pivaloyloxymethyl phosphonodiester of pentachlorophenyl 4-phosphonodifluoromethylcinnamate, a phosphotyrosine surrogate, was synthesized and used to acylate peptidomimetic fragments that were...
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PMID: 19594124
PDF is available here.
PDF is available here.
Journal of Organic Chemistry (74)15 2009
Chiral Base-Catalyzed Enantioselective Synthesis of 4-Aryloxyazetidinones and 3,4-Benzo-5-oxacephams
Abstract
Readily available 4-formyloxyazetidinone was enantioselectively transformed into 3,4-benzo-2-hydroxy-5-oxacephams and 4-phenyloxyazetidinones upon treatment with 0.1 equiv of the cinchona alkaloid in toluene via intermolecular nucleophilic trapping of N-acyliminium intermediate by the hydroxyl moiet...
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PMID: 19572576
PDF is available here.
PDF is available here.
Journal of Organic Chemistry (74)15 2009
Abstract
Six antitumor antibiotics of a new structure class, indoxamycins A-F (1-6), were isolated from a saline culture group of marine-derived actinomyces whose strains showed approximately 96% sequence homology of 16S rDNA with the family streptomycetaceae. The structures of these indoxamycins, which are...
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PMID: 19572603
PDF is available here.
PDF is available here.
Abstract
Brønsted acid promoted reversible dimerization of myrmicarin 215B leads to formation of a new heptacyclic product, isomyrmicarin 430B, that possesses a C1,C2-trans,C2,C3-trans-substituted cyclopentane ring. Mechanistic studies illustrate that isomyrmicarin 430B arises by isomerization of isomyrmica...
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PMID: 19586059
PDF is available here.
PDF is available here.
Abstract
Two new Lycopodium alkaloids, serratezomines D (1) and E (2), were isolated from the club moss Lycopodium serratum var. serratum. Serratezomine D (1) is a new lucidine-type alkaloid, while serratezomine E (2) is a new phlegmarane-type alkaloid. The structures and relative stereochemi...
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PMID: 19447614
PDF is available here.
PDF is available here.
Journal of Ethnopharmacology (123)3 2009
Abstract
Ethyl acetate extract showed promising antibacterial and antifungal activity and isolated compound Flindersine showed moderate activity against bacteria and fungi....
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PMID: 19481384
PDF is available here.
PDF is available here.
Abstract
The enantioselective total synthesis of the potent alpha-glucosidase inhibitors schulzeine A, B, and C and a revision of the proposed C20' configuration of schulzeine A are reported. The central feature of our convergent route to this family of novel marine natural products is the preparation of the...
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PMID: 19361223
PDF is available here.
PDF is available here.
Journal of Antibiotics (62)5 2009
Abstract
Streptomyces griseoviridis 2464-S5 produces prodigiosin R1, a tripyrrole antibiotic, and roseophilin, a structurally related compound containing two pyrrole and one furan rings. A gene cluster for the biosynthesis of a prodigiosin was identified in S. griseoviridis. The cluster consisted of 24 open...
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PMID: 19329986
PDF is available here.
PDF is available here.
Abstract
Tris-(p-carboxyltetrathiaaryl)methyl radical EPR probes are very efficiently oxidized by superoxide and alkylperoxyl radicals with selective formation of quinone-methide products; this should explain the previously reported specific measurement of O2*- using these EPR probes.
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PMID: 19259606
PDF is available here.
PDF is available here.
Abstract
We hypothesized that inhibition of the intracellular NF-kappaB pathway in alloreactive T-cells, which is critical for T-cell activation events including IL-2 transcription, could lead to alloantigen hyporesponsiveness and loss of GVHD capacity. We demonstrate that treatment of mixed lymphocyte react...
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PMID: 19260829
PDF is available here.
PDF is available here.
Abstract
A very simple strategy for the construction of 2,3-benzofused 8-oxabicyclo[3.2.1]octane derivatives is reported. This new process is based on a platinum-catalyzed tandem intramolecular hydroalkoxylation-hydroarylation reaction of aryl-substituted pentynol derivatives. This reaction has been applied...
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PMID: 19143035
PDF is available here.
PDF is available here.
Abstract
The purpose of this study was to determine whether AVE7688 a drug that inhibits both angiotensin converting enzyme and neutral endopeptidase activity protects vascular and nerve functions in an animal model of metabolic syndrome. Obese Zucker rats at 20 weeks of age were treated for 12 weeks with AV...
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PMID: 19536347
PDF is available here.
PDF is available here.
Abstract
Of 454 RA patients identified, 212 have been on a biologic agent at one point in time, and 100 patients (47%) had either stopped or switched their first biologic agent. Among these 100 patients, the most common reasons for stopping or switching a biologic agent were adverse events (in 48%) and ineff...
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PMID: 20149307
PDF is available here.
PDF is available here.
BMC Neuroscience (10)1 2009
Abstract
To gain insights into the molecular mechanisms of SOD1(G93A) associated motor neuron disease, we simultaneously monitored cytosolic and mitochondrial calcium concentrations in individual cells. Voltage - dependent cytosolic Ca2+ elevations and mitochondria - controlled calcium release mechanisms wer...
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PMID: 19545440
PDF is available here.
PDF is available here.
Abstract
Abstract
Abstract
Fast and furious: Cribrostatin 6, an antimicrobial and antineoplastic agent, was the target of a total synthesis where the longest linear sequence was only four steps. The key step involves a tandem 4pi electrocyclic ring opening, radical cyclization, and homolytic aromatic substitution sequence to...
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PMID: 19235818
PDF is available here.
PDF is available here.
Abstract
I DNA unwinding (Topo I) assay. The dyes of this study showed tight binding to ctDNA with binding constants, K(b), on the order of 10(6)-10(7)M(-1). The ITC and Topo I assay studies suggested that the 9-substituent has a strong impact on binding modes ranging from an apparent preference for intercal...
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PMID: 18993079
PDF is available here.
PDF is available here.
Abstract
2,6-Bis(tert-butyldimethylsilyloxy)-9-oxabicyclo[3.3.1]nonane-3,7-diol, C(20)H(42)O(5)Si(2), (I), and 4,8-bis(tert-butyldimethylsilyloxy)-2,6-dioxatricyclo[3.3.1(3,7)]decane-1,3-diol, C(20)H(40)O(6)Si(2), (II), form layered structures that differ in the way the molecules are connected within each la...
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PMID: 19057079
PDF is available here.
PDF is available here.
Abstract
New fungal metabolites, designated quinadolines A (1) and B (2), were isolated from culture broth of Aspergillus sp. FKI-1746, and their structures were elucidated by NMR spectroscopy. The complete relative and absolute stereochemistry of 2 was determined by X-ray crystallography and amino acid anal...
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PMID: 18922003
PDF is available here.
PDF is available here.
Abstract
A series of novel tricyclic triazine-di- N-oxides (TTOs) related to tirapazamine have been designed and prepared. A wide range of structural arrangements with cycloalkyl, oxygen-, and nitrogen-containing saturated rings fused to the triazine core, coupled with various side chains linked to either he...
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PMID: 18847185
PDF is available here.
PDF is available here.
Gastroenterology (135)5 2008
Abstract
NS3/4A protease inhibitors can restore IRF-3 signaling in HCV-infected cells but only at concentrations far in excess of the antiviral EC(50)....
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PMID: 18725224
PDF is available here.
PDF is available here.
Abstract
We first studied the [Ca2+]c and mitochondrial matrix Ca2+ ([Ca2+]m) signals in single preglomerular afferent arteriolar smooth muscle cells (PGASMC). TGF-beta pretreatment (24 h) decreased both the [Ca2+]c and [Ca2+]m responses evoked by angiotensin II or endothelin. Strikingly, the [Ca2+]m signal...
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PMID: 18653477
PDF is available here.
PDF is available here.
Abstract
We discuss some of the most common chemical Ca2+ indicators that are widely used for the investigation of intracellular Ca2+ signaling. Advantages, limitations and relevant procedures will be presented for each dye including their spectral qualities, dissociation constants, chemical forms, loading m...
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PMID: 18929663
PDF is available here.
PDF is available here.
Biochimica et Biophysica Acta (1782)9 2008
Abstract
We hypothesize that these differences between oligomers and fibrils are related to their different accessibility to the intracellular space. To this end we used fluorescently labelled Abeta1-42 and demonstrate that Abeta1-42 oligomers readily enter both HeLa and differentiated SKNSH cells whereas fi...
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PMID: 18602001
PDF is available here.
PDF is available here.
Abstract
Chemical investigations on the sea whip gorgonian coral Junceella juncea have led to the isolation of five new 8-hydroxybriarane diterpenoids, junceols D-H (1-5). The structures of briaranes 1-5 were determined on the basis of spectroscopic methods and the methylenecyclohexane rings were found to ex...
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PMID: 18758100
PDF is available here.
PDF is available here.
Abstract
We recently reported that K13 antagonizes KSHV lytic regulator RTA (replication and transcription activator) and blocks lytic replication, but spares RTA-induced viral interleukin-6 (vIL6). Here we report that K13 is also present in the nuclear compartment, a property not shared by its structural ho...
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PMID: 18469854
PDF is available here.
PDF is available here.
Abstract
SAR analysis performed with a limited set of cyclopentane-containing macrocycles led to the identification of N-[17-[2-(4-isopropylthiazole-2-yl)-7-methoxy-8-methylquinolin-4-yloxy]-13-methyl-2,14-dioxo-3,13-diazatricyclo [13.3.0.0(4,6)]octadec-7-ene-4-carbonyl](cyclopropyl)sulfonamide (TMC435350, 3...
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PMID: 18678486
PDF is available here.
PDF is available here.
Abstract
Three phlorotannins, including phloroglucinol, diphlorethohydroxycarmalol, and 6,6'-bieckol, were isolated from Ishige okamurae by column chromatography. The structures of the phlorotannins were determined on the basis of spectroscopic analysis, including NMR and mass spectrometry (MS) techniques. A...
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PMID: 18616277
PDF is available here.
PDF is available here.
Abstract
Our synthetic route provided a range of key analogues with partial structures to define the pharmacophore. Simplification of the caprazamycins was further pursued to develop diketopiperazine analogs....
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PMID: 18670104
PDF is available here.
PDF is available here.
Leukemia & Lymphoma (49)8 2008
Abstract
Non-steroidal anti-inflammatory drugs (NSAIDs) comprise the group of structurally diverse but similarly acting compounds that are used for relieving signs and symptoms of inflammation, especially in treatment of rheumatic diseases. Recent reports suggested potential association between regular use o...
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PMID: 18608871
PDF is available here.
PDF is available here.
Abstract
The MEK inhibitor PD0325901 has a wide range of potent inhibitory effects on thyroid cancer cells, some of which seemed to be genotype-selective, consistent with the results previously observed with an early-generation MEK inhibitor, CI-1040. The data provide further evidence that targeted inhibitio...
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PMID: 18651802
PDF is available here.
PDF is available here.
Journal of Organic Chemistry (73)14 2008
Abstract
Total syntheses of cassiarins A and B have been efficiently accomplished using a common strategy with biomimetic considerations. Key reactions involved in this synthesis include a Negishi-type coupling, a Ag(I)-promoted formation of the tricyclic 8H-pyrano[2,3,4-de]chromen-8-one core, and a sequenti...
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PMID: 18570405
PDF is available here.
PDF is available here.
Abstract
One new compound 6-demethylvermistatin (1), together with two known compounds, the penicillide derivatives (2) and (3) were isolated from the mangrove fungus Guignardia sp. No. 4382 obtained from the South China Sea. Their structures were assigned using high-resolution electron ionization mass spect...
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PMID: 18338749
PDF is available here.
PDF is available here.
Abstract
Roseophilin is a unique metabolite containing two pyrrole and one furan ring and is structurally related to tripyrrole antibiotics, prodigiosins. Each homologous gene in the roseophilin producer Streptomyces griseoviridis was amplified by PCR using primers designed from the prodigiosin-biosynthesis...
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PMID: 18553921
PDF is available here.
PDF is available here.
Abstract
A new bischromone, chrobisiamone A (1) with an antiplasmodial activity has been isolated from the leaves of Cassia siamea and the structure was elucidated by 2D NMR analysis. Cyclization of 5-acetonyl-7-hydroxy-2-methylchromone (2) in the presence of ammonium acetate resulted in generation of cassia...
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PMID: 18524594
PDF is available here.
PDF is available here.
Abstract
Consensus virtual screening models were generated and validated utilizing a set of known human epidermal growth factor receptor-2 (HER2) inhibitors and modeled HER2 active and inactive state structures. The virtual screening models were successfully employed to discover a set of structurally diverse...
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PMID: 18500794
PDF is available here.
PDF is available here.
European Journal of Pharmacology (586)1-3 2008
Abstract
The effect of tournefolic acid B (TAB) on amyloid beta protein-mediated neurotoxicity and the underlying mechanisms were investigated. Amyloid beta protein 25-35 elicited neuronal death as determined by calcein/ethidium homodimer-1 staining. 10 microM amyloid beta protein 25-35 caused cell death at...
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PMID: 18374914
PDF is available here.
PDF is available here.
Mutation Research (653)1-2 2008
Abstract
Three structurally related phenyltetrahydropyridinyl butylazole (PTHPB)-derived drug candidates with sigma receptor-binding properties were evaluated for genotoxic potential in the ICH standard battery of genetic toxicology assays. These comprised an Ames test, a mouse-lymphoma assay, and a mouse bo...
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PMID: 18502168
PDF is available here.
PDF is available here.
Electrophoresis (29)11 2008
Abstract
1,4,10,13,16-Pentaazatricycloheneicosane-9,17-dione (macrocyclic polyamine)-modified polymer-based monolithic column for CEC was prepared by ring opening reaction of epoxide groups from poly(glycidyl methacrylate-co-ethylene dimethacrylate) (GMA-co-EDMA) monolith with macrocyclic polyamine. Conditio...
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PMID: 18446806
PDF is available here.
PDF is available here.
Abstract
From the Egyptian medicinal plant Polygonum senegalense the fungal endophyte Alternaria sp. was isolated. Extracts of the fungus grown either in liquid culture or on solid rice media exhibited cytotoxic activity when tested in vitro against L5178Y cells. Chromatographic separation of the extracts yi...
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PMID: 18494522
PDF is available here.
PDF is available here.
Abstract
Pestaloficiols A-E (1-5), five new cyclopropane derivatives, have been isolated from cultures of the plant endophyte Pestalotiopsis fici. The structures of these compounds were determined by NMR spectroscopy, and the absolute configuration of 1 was assigned using the modified Mosher method. Compound...
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PMID: 18468908
PDF is available here.
PDF is available here.
Organic Letters (10)10 2008
Abstract
The first total synthesis of cassiarin A, an antiplasmodial alkaloid isolated from Cassia siamea, was achieved via sequential alkynylation of arenes with Sonogashira coupling and 6- endo-dig-cyclization of phenolic oxygens to the resulting alkynes.
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PMID: 18412353
PDF is available here.
PDF is available here.
Bioconjugate Chemistry (19)5 2008
Abstract
We report the synthesis of a novel conjugate between a near-infrared indocyanine dye and an organic polyamine polymer (polyethylenimine, PEI) (IR820-PEI) with high chemical stability and good optical properties. IR820-PEI absorbs at 665 nm, emits at 780 nm, and displays a large Stokes shift (115 nm)...
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PMID: 18429627
PDF is available here.
PDF is available here.
Abstract
Three-dimensional quantitative structure-activity relationship (3D-QSAR) models were developed for 46 triazafluorenone derivatives, inhibiting metabotropic glutamate receptor subtype 1 (mGluR1). It includes molecular field analysis (MFA) and receptor surface analysis (RSA). The QSAR model was develo...
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PMID: 17822809
PDF is available here.
PDF is available here.