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Heterocyclic Compounds (9):
Recent article
Heterocyclic Compounds
Organic Letters (13)18 2011
Abstract
Asymmetric vinylogous Mannich reaction (VMR) of 2-(tert-butyldimethylsilyloxy)furan (TBSOF, 1) with (R(S))- or (S(S))-t-BS-imines (3) furnished 5-aminoalkylbutenolides 7a-k in 75-87% yields with anti/syn ratios ranging from 75:25 to 97:3. Butenolides 7a-f,k were readily converted int...
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PMID: 21854016
PDF is available here.
PDF is available here.
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Bulletin du cancer (98)8 2011
Abstract
Mobilization is the biological phenomenon by which hematopoietic stem and progenitor cells (HSPC) transiently egress the bone marrow compartment and circulates in peripheral blood. The biological significance of this phenomenon is incompletely understood, although it is likely to be...
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PMID: 21835729
PDF is available here.
PDF is available here.
Organic Letters (13)7 2011
Abstract
The (hetero)aromatic trifluoromethyl group is present in many biologically active molecules and is generally considered to be chemically stable. In this paper, a convenient one-step synthesis of C-C linked aryl-heterocycles or heteroaryl-heterocycles in good to excellent yields via t...
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PMID: 21381681
PDF is available here.
PDF is available here.
Abstract
Our recent in vitro study demonstrated that endothelial cells (ECs) might influence the differentiation of bone marrow stromal cells (BMSCs). Therefore, the aim of this study was to describe this effect in vivo, using a rat calvarial bone defect model. BMSCs were isolated from femurs of two-donor Le...
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PMID: 21171154
PDF is available here.
PDF is available here.
Metallomics (3)1 2011
Abstract
From the reaction of 1-methylimidazole (1a), 4,5-dichloro-1H-imidazole (1b(I)) and 1-methylbenzimidazole (1c) with p-cyanobenzyl bromide (2a), non-symmetrically substituted N-heterocyclic carbene (NHC) [(3a-c)] precursors, 5,6-dimethyl-1H-benzimidazole (1d) and 4,5-diphenyl-1H-imidaz...
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PMID: 21135954
PDF is available here.
PDF is available here.
Abstract
Abstract
(Spectro-)electrochemical results demonstrate ligand-centred hydride ion-carrier capacity for a Rh(I) complex of a novel 'non-innocent' N-heterocyclic carbene ligand created by nicotinamide functionalisation.
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PMID: 20922240
PDF is available here.
PDF is available here.
Chemical Communications (46)42 2010
Abstract
We report that apo-cyclen, attached to a specific hIAPP recognition motif (NYGAIL), captured copper ions and became proteolytically active. This cyclen-NYGAIL-copper complex was able to interfere with hIAPP aggregation and cleave hIAPP. These activities rescued INS-1 cells from hIAPP induced cytotox...
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PMID: 20856987
PDF is available here.
PDF is available here.
Organic Letters (12)21 2010
Abstract
The gas-phase proton affinities of unusually basic phosphines and N-heterocyclic carbenes are compared and contrasted both computationally and experimentally.
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PMID: 20886843
PDF is available here.
PDF is available here.
Chemical Communications (46)40 2010
Abstract
Metal-free deprotonative functionalization of heteroaromatic compounds was achieved using an organic superbase catalyst; an organosilicon additive such as trimethylsilylpropyne was employed for activating the catalytic cycle of 1,2-addition to carbonyl compounds.
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PMID: 20848038
PDF is available here.
PDF is available here.
Chemical Communications (46)40 2010
Abstract
C(1)-symmetric isoquinoline-based chiral diaminocarbene ligands (MIQ) have been developed to block three quadrants of the metal coordination sphere, complementing C(2)-symmetric biisoquinoline-based ligands (BIQ). MIQ-Cu complexes catalyzed conjugate borylation of various α,β-unsaturated amides in...
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PMID: 20835472
PDF is available here.
PDF is available here.
Biochemical Journal (432)1 2010
Abstract
We have developed a high-content assay for human embryonic stem cell survival and used this to screen a range of libraries of 'lead-like' small molecules and known bioactives. From this we identified 18 confirmed hits with four structural classes being represented by multiple compounds: a series of...
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PMID: 20854259
PDF is available here.
PDF is available here.
Abstract
We demonstrated that a prolonged therapy with phosphodiesterase-5 (PDE5) inhibitors does improve endothelial function and increases circulating EPC, suggesting a role of PDE5 in EPC physiology. Here we tested the expression of PDE5 and CXCR4 on cultured, circulating, and bone marrow resident EPC, an...
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PMID: 20695838
PDF is available here.
PDF is available here.
Chemical Communications (46)34 2010
Abstract
A highly efficient silver triflate and N-heterocyclic carbene co-catalyzed three-component reaction of N'-(2-alkynylbenzylidene)hydrazide, methanol with alpha,beta-unsaturated aldehyde is described, which gives rise to the 2-amino-1,2-dihydroisoquinolines in good yield.
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PMID: 20697636
PDF is available here.
PDF is available here.
Abstract
We present an introduction to TB, followed by an overview of new heterocyclic anti-tubercular moieties published during the last decade....
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PMID: 21426140
PDF is available here.
PDF is available here.
Abstract
The collision-induced dissociations are reported for Cu(II) complexes containing 1,4,7-triazacyclononane (tacn) as the auxiliary ligand and a peptide containing one cystine residue. For six of the complexes examined, cleavage of the S-S bond in the peptide was the dominant fragmentation pathway. The...
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PMID: 20539872
PDF is available here.
PDF is available here.
Abstract
The anion binding ability of bis-zinc cyclen complexes in buffered aqueous solution was investigated using indicator displacement assays (IDA) as well as luminescent labelled complexes. A high affinity to phosphate anions, such as UTP or pyrophosphate was observed in IDA while there was no observabl...
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PMID: 20559585
PDF is available here.
PDF is available here.
Abstract
Our data support the use of Gd and MRI to monitor AAV2 infusion via CED and to predict the distribution of GDNF protein after AAV2-GDNF administration....
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PMID: 20551915
PDF is available here.
PDF is available here.
Journal of Neurosurgery (113)2 2010
Abstract
The present study provides quantitative analysis of cannula placement and infusate distribution using real-time MR imaging and defines an optimal zone for infusion in the nonhuman primate thalamus and brainstem. Cannula placement recommendations developed from such translational nonhuman primate stu...
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PMID: 20367078
PDF is available here.
PDF is available here.
Abstract
Phenylpyridal- and phenyldipyridal-based scaffolds have been designed and synthesized as novel helical peptide mimetics. The synthesis required optimisation and selective alkylation in producing 2,6-functionalized 3-hydroxypyridine derivatives for a convergent scheme. The pyridine analogues were cou...
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PMID: 20564292
PDF is available here.
PDF is available here.
Abstract
Systematic studies are presented demonstrating the complementarity of directed ortho metalation (DoM) and Ir-catalyzed strategies for the provision of borylated aromatics and their subsequent Suzuki-Miyaura coupling reactions. A new concept, the use of the TMS group, readily introduced by DoM, as a...
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PMID: 20533457
PDF is available here.
PDF is available here.
Abstract
PURPOSE. Endothelial precursor cells (EPCs) derived from hematopoietic stem cells (HSCs) have been shown to contribute to choroidal neovascularization by signaling through the SDF-1/CXCR4 axis. In a prevention and treatment/intervention modality of the laser choroidal neovascularization (CNV) model,...
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PMID: 20042641
PDF is available here.
PDF is available here.
Abstract
AMD3100 is a bicyclam molecule that selectively and reversibly antagonizes the binding of stromal cell-derived factor-1 (SDF-1) to its receptor CXC motif receptor-4 (CXCR4) with subsequent egress of hematopoietic stem cells to the peripheral blood. AMD3100 safely and rapidly mobilizes stem cells in...
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PMID: 20473162
PDF is available here.
PDF is available here.
Abstract
We studied the effects of AMD3100, CXCR4 antagonist, on a murine bleomycin-induced pulmonary fibrosis model. Treatment of mice with AMD3100 in bleomycin-treated mice resulted in the decrease of SDF-1 in bronchoalveolar lavage (BAL) fluids at an early stage and was followed by the decrease of fibrocy...
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PMID: 20498529
PDF is available here.
PDF is available here.
Abstract
We hypothesized that a small molecule CXCR4 antagonist, AMD3100 (AMD), could augment the mobilization of bone marrow (BM)-derived endothelial progenitor cells (EPCs), thereby enhancing neovascularization and functional recovery after myocardial infarction. Single-dose AMD injection administered afte...
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PMID: 20534467
PDF is available here.
PDF is available here.
Anticancer Research (30)6 2010
Abstract
The increasing number of stem cells found in tumor spheroids over time is attributed to cell recruitment. Stem cell migration in vitro was enhanced by exogenous SDF1 and abrogated by CXCR4 inhibition and. CXCR4 inhibition reduced tumor burden in vivo. CONCLUSION: SDF1 is a candidate chemokine for re...
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PMID: 20651364
PDF is available here.
PDF is available here.
Anticancer Research (30)6 2010
Abstract
Only CXCR4 mRNA levels in gastric cancer tissues were correlated with docetaxel sensitivity (R(2)=0.23, p=0.019) and significantly higher in resistant specimens (p=0.038). AMD3100, a CXCR4 antagonist, enhanced the docetaxel cytotoxicity in vitro. CONCLUSION: CXCR4 mRNA expression levels may be a pot...
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PMID: 20651371
PDF is available here.
PDF is available here.
Abstract
Abstract
CuO nanoparticles provide an efficient, economic, and novel method for the synthesis of quinoxaline, benzoxazine, and benzothiazine under ultrasonic irradiation. The protocol offers advantages in terms of higher yields, short reaction times, and mild reaction conditions, with reusability of the cata...
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PMID: 20299269
PDF is available here.
PDF is available here.
Abstract
The compounds were found to inhibit growth of both cell lines in a dose-dependent manner and also showed selective cytotoxicity against the cancer cells when compared with normal peripheral blood mononuclear cells. Growth suppression by these compounds was due to apoptosis, as evidenced by the cell...
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PMID: 20458760
PDF is available here.
PDF is available here.
Abstract
It has been shown that various pyrido-, quinolino-, pyrazino-, and quinoxalinotetrazoles can be used efficiently as azide components in Cu-catalyzed click reaction with alkynes. This method allows for efficient synthesis of a wide variety of N-heterocyclic derivatives of 1,2,3-triazoles.
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PMID: 20380424
PDF is available here.
PDF is available here.
Abstract
The strong directing ability of the N,N,N',N'-tetramethyldiaminophosphorodiamidate group has been used to achieve selective metalations on various heterocycles such as pyridines, quinolines and quinoxalines with TMP-derived bases like TMPMgCl x LiCl, TMP(2)Mg x 2 LiCl, and TMP(2)Zn x 2 MgCl(2) x 2 L...
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PMID: 20356104
PDF is available here.
PDF is available here.
Abstract
We established that interaction of the aryl-substituted epoxyimides of norbornane with sodium ethoxide results in the formation of new heterocyclic compounds in preparatively useful yields and with complete regioselectivity. The reactions of epoxyimides, containing aryl electron-donor substituents,...
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PMID: 20401391
PDF is available here.
PDF is available here.
Abstract
Thiol-Olefin Co-Oxygenation (TOCO) methodology has been applied to the synthesis of a small library of weak base and polar 1,2,4-trioxanes. The 1,2,4-trioxane units synthesised exhibit remarkable stability as they survive base catalysed hydrolysis and mixed anhydride/amine coupling reactions. This u...
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PMID: 20401383
PDF is available here.
PDF is available here.
Abstract
We report a reagent-based, diversity-oriented synthetic (DOS) strategy to probe chemical and biological space via a "Click, Click, Cyclize" protocol. In this DOS approach, three sulfonamide linchpins underwent cyclization protocols with a variety of reagents to yield a collection of structurally div...
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PMID: 20401396
PDF is available here.
PDF is available here.
Clinical Therapeutics (32)5 2010
Abstract
Autologous hematopoietic stem cell (HSC) transplantation is used to facilitate hematopoietic recovery after administration of high-dose chemotherapy in patients with Hodgkin's disease, non-Hodgkin's lymphoma (NHL), multiple myeloma (MM), leukemias, and some solid tumors. There are limitations to the...
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PMID: 20685493
PDF is available here.
PDF is available here.
Investigative Radiology (45)5 2010
Abstract
For both groups of animals, after an initial increase, a transient decay of the longitudinal relaxation rate was observed, followed by a constant plateau after 20 minutes. The analysis of the mean relaxation rates in the liver showed significant (P < 0.01) higher values for the group with destructio...
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PMID: 20375844
PDF is available here.
PDF is available here.
Abstract
Three different types of homobivalent compounds, 5,8,9,13b-tetrahydro-6H-isoqino[1,2-a]isoquinolines bearing tertiary N-atoms, their quaternary ammonium salts and their dibenzazecine analogues, connected by alkylene spacers of various lengths were synthesized. Compared to the therapeutically used in...
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PMID: 20350808
PDF is available here.
PDF is available here.
European Radiology (20)5 2010
Abstract
Comprehensive CMR provides accurate assessment of IS and MAR in reperfused rabbit MI. Infarct size is closely related to LV remodelling. Through the infarct size/MAR ratio, this approach has great potential for assessing interventions aimed at cardioprotection....
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PMID: 19936756
PDF is available here.
PDF is available here.
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.
PDF is available here.
Abstract
Using 3-methyl-4-phenylthieno[2,3-b]thiophene-2,5-dicarbohydrazide as synthon a series of new bis-heterocycles incorporating the thieno[2,3-b]thiophene nucleus was prepared and characterized.
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PMID: 20657483
PDF is available here.
PDF is available here.
Molecular Diversity (14)2 2010
Abstract
The 1:1 zwitterionic intermediates obtained from the reaction between isoquinoline, quinoline, pyridine, or N-methylimidazole with activated acetylenes are trapped by ethyl pyruvate to produce highly functionalized fused [1,3]oxazines in good yields.
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PMID: 19578943
PDF is available here.
PDF is available here.
Abstract
N,N'-Di-4-triazolylurea (DTU) has developed as a new ADDA module and DTU forms a stable ADDA*DAAD heterocomplex with 2,7-diamido-1,8-naphthyridine (DAN) (K(s) = 2.6 x 10(5) M(-1) in CHCl(3)). The K(s) value of the complex between DTU and DAN is 100-fold greater than that of the complex between N,N'-...
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PMID: 20232854
PDF is available here.
PDF is available here.
Abstract
Functionalization of polyanthranilic acid (PAA) a self-doped conducting polymer with Co(II) metal complex has been reported and is used in the development of azidothymidine drug sensor. For the first time synthesis of a new type of polymer complex of Co(II)-cyclam macrocyclic ligand (1,4,8,11-tetraa...
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PMID: 20188945
PDF is available here.
PDF is available here.
The Journal of Chemical Physics (132)15 2010
Abstract
Our analysis demonstrates the tremendously importance of some specific exchange mechanisms. It is actually shown that both parts of the imvdz ligand simultaneously influence the ferromagnetic behavior which ultimately reaches J(calc)=6.3 cm(-1), in very good agreement with the experimental value. In...
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PMID: 20423193
PDF is available here.
PDF is available here.
Abstract
We assigned to changes occurring in the coordination environment of the ion within the cyclen system, caused by deprotonation of metal bound water molecules and/or deprotonation of pendent amide arms....
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PMID: 20354617
PDF is available here.
PDF is available here.
Chemical Communications (46)14 2010
Abstract
Photoliberation of a caged, chelating naphthalene antenna greatly enhances the luminescence of a Eu(III)-cyclen complex due to metal-bound water displacement and sensitization by the antenna, giving a lanthanide-labelling strategy in different media, being optimal in the presence of a TMADS surfacta...
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PMID: 20379558
PDF is available here.
PDF is available here.
Abstract
These results show that the transport of carriers in the neutral unicomponent radical crystal can be controlled by the external magnetic field. These findings are important as a basis for developing molecule-based spin electronic devices....
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PMID: 20222711
PDF is available here.
PDF is available here.
Clinical Cancer Research (16)7 2010
Abstract
EGFR expression on UM-SCC-22B cells is lower than that on SCC1 cells. However, the UM-SCC-22B tumors showed much higher (64)Cu-DOTA-cetuximab accumulation than the SCC1 tumors. Cetuximab-induced apoptosis in SCC1 tumors and tumor growth was significantly inhibited, whereas an agonistic effect of cet...
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PMID: 20215534
PDF is available here.
PDF is available here.
Abstract
An efficient method for the synthesis of symmetrical and unsymmetrical substituted thiourea derivatives by means of simple condensation between available building blocks such as amines and carbon disulfide in aqueous medium is presented. This protocol works smoothly with aliphatic primary amines to...
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PMID: 20201494
PDF is available here.
PDF is available here.
Abdominal Imaging (35)2 2010
Abstract
Contrast-enhanced ultrasonography diagnosis was concordant with MR or CT images in all cases. Conclusion: In our experience CEUS shows complete concordance with CT and MRI in the characterization of all 24 pseudotumors considered dubious at conventional and power Doppler US. The appropriate use of C...
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PMID: 19194642
PDF is available here.
PDF is available here.
Abstract
A series of imidazolidinium ligand precursors are metallated with Ag2O to give silver(I) N-heterocyclic carbene complexes. All compounds were fully characterized by elemental analyses, 1H-NMR, 13C-NMR and IR spectroscopy techniques. All compounds studied in this work were screened for their in vitro...
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PMID: 20428059
PDF is available here.
PDF is available here.
Abstract
The synthesis of the title compounds was achieved using ethyl 2-amino-6-methyl-4,5,6,7-tetrahydrothieno[2,3-c]pyridine-3-carboxylate (1) as starting material. The reaction of the amino ester 1 with phenylisothiocyanate in boiling ethanol afforded the thiourea derivative 5. The cyclization reactions...
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PMID: 20428071
PDF is available here.
PDF is available here.
Abstract
CHI's 17th International Tri-Conference on Molecular Medicine, held in San Francisco, included topics covering the drug discovery process, with an emphasis on lead optimization. This conference report highlights selected presentations on the development of several launched and investigational drugs,...
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PMID: 20373246
PDF is available here.
PDF is available here.
Abstract
We report a one-pot, iridium-catalyzed, silyl-directed C-H borylation of indoles at the 7-position. This process occurs in high yield with a variety of substituted indoles, and conversions of the 7-borylindole products to 7-aryl-, 7-cinnamyl-, and 7-haloindoles are demonstrated. The Ir-catalyzed, si...
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PMID: 20199022
PDF is available here.
PDF is available here.
Abstract
We show that these differences allow the enzymes to control regioselectivity of posttranslational modifications, helping to control product chemistry in this hypervariable family of marine natural products....
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PMID: 20210311
PDF is available here.
PDF is available here.
Abstract
We conveniently established reactive alpha-halomethylene compounds, aldehydes and beta-dicarbonyl compounds a library of zwitterionic salts....
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PMID: 20092329
PDF is available here.
PDF is available here.
Abstract
Abstract