- Fuel-Selective Transient Activation of Nanosystems for Signal Generation
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The transient activation of function using chemical fuels is common in nature, but much less in synthetic systems. Progress towards the development of systems with a complexity similar to that of natural ones requires chemical fuel selectivity. Here, we show that a self-assembled nanosystem, composed of monolayer-protected gold nanoparticles and a fluorogenic peptide, is activated for transient signal generation only in case the chemical fuel matches the recognition site present at the nanoparticle surface. A modification of the recognition site in the nanosystem completely changes the chemical fuel selectivity. When two nanosystems are simultaneously present, the selectivity expressed by the system depends on the concentration of nucleotide added.
- della Sala, Flavio,Maiti, Subhabrata,Bonanni, Andrea,Scrimin, Paolo,Prins, Leonard J.
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- A selective inhibitor of the UFM1-activating enzyme, UBA5
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Protein conjugation with ubiquitin and ubiquitin-like small molecules, such as UFM1, is important for promoting cancer cell survival and proliferation. Herein, the development of the first selective micromolar inhibitor of the UBA5 E1 enzyme that initiates UFM1 protein conjugation is described. This organometallic inhibitor incorporates adenosine and zinc(II)cyclen within its core scaffold and inhibits UBA5 noncompetitively and selectively over other E1 enzymes and a panel of human kinases. Furthermore, this compound selectively impedes the cellular proliferation (above 50?μM) of cancer cells containing higher levels of UBA5. This inhibitor may be used to further probe the intracellular role of the UFM1 pathway in disease progression.
- da Silva, Sara R.,Paiva, Stacey-Lynn,Bancerz, Matthew,Geletu, Mulu,Lewis, Andrew M.,Chen, Jijun,Cai, Yafei,Lukkarila, Julie L.,Li, Honglin,Gunning, Patrick T.
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- Dinuclear macrocyclic polyamine zinc(II) complexes linked with flexible spacers: Synthesis, characterization, and DNA cleavage
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Dinuclear macrocyclic polyamine zinc(II) complexes, which have two cyclen groups linked by flexible spacers, have been synthesized as DNA cleavage agents. The structures of these new dinuclear complexes are consistent with the data obtained from elemental analysis, MS and 1H NMR spectroscopy. The catalytic activity of these dinuclear complexes on DNA cleavage was studied. The results showed that the dinuclear zinc(II) complexes can catalyze the cleavage of supercoiled DNA (pUC 19 plasmid DNA) (Form I) under physiological conditions to produce selectively nicked DNA (Form II).
- Peng, Wei,Liu, Pei-Yan,Jiang, Ning,Lin, Hong-Hui,Zhang, Guo-Lin,Liu, Yi,Yu, Xiao-Qi
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- Chiral multinuclear macrocyclic polyamine complexes: Synthesis, characterization and their interaction with plasmid DNA
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A series of multinuclear macrocyclic polyamine metal (Zn2+, Cu2+, Co2+) complexes containing chiral dipeptide linkage were synthesized and used as artificial nuclease enzyme model. The interaction between the complexes and
- Fang, Yu-Guo,Zhang, Ji,Chen, Shan-Yong,Jiang, Ning,Lin, Hong-Hui,Zhang, Yu,Yu, Xiao-Qi
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- Synthesis of calix[4]arene-cyclen conjugates
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Novel calix[4]arene derivatives constrained in the cone or 1,3-alternate conformations, bearing one or two cyclen (1,4,7,10-tetraazacyclododecane) moieties directly connected to the upper rim, have been synthesized using Buchwald-Hartwig coupling reaction. The complexation ability and hydrolytic activities of selected Zn(II) complexes of these calixarenes were studied. Although the attempts to hydrolyze activated phosphodiester bonds were unsuccessful, the NMR titration experiments revealed binding affinity for chloride, acetate, and benzoate anions in defined stoichiometry.
- Stastny, Václav,Lhoták, Pavel,Stibor, Ivan,K?nig, Burkhard
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- 5-HT1A targeting PARCEST agent DO3AM-MPP with potential for receptor imaging: Synthesis, physico-chemical and MR studies
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Contrast enhancement in MRI using magnetization or saturation transfer techniques promises better sensitivity, and faster acquisition compared to T1 or T2 contrast. This work reports the synthesis and evaluation of 5-HT1A
- Anju,Chaturvedi, Shubhra,Chaudhary, Vishakha,Pant, Pradeep,Jha, Preeti,Kumaran, Senthil S.,Hussain, Firasat,Kumar Mishra, Anil
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- Vesicles and micelles from amphiphilic Zinc(II)-cyclen complexes as highly potent promoters of hydrolytic DNA cleavage
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Phosphate esters are essential to any living organism and their specific hydrolysis plays an important role in many metabolic processes. As phosphodiester bonds can be extraordinary stable, as in DNA, great effort has been put into mimicking the active sites of hydrolytic enzymes which can easily cleave these linkages and were often found to contain one or more coordinated metal ions. With this in mind, we report micellar and vesicular Zn(II)-cyclen complexes which considerably promote the hydrolytic cleavage of native DNA and the activated model substrate bis(4-nitrophenyl)phosphate (BNPP). They are formed by self-assembly from amphiphilic derivatives of previously employed complexes in aqueous solution and therefore allow a simple and rapid connection of multiple active metal sites without great synthetic effort. Considering the hydrolytic cleavage of BNPP at 25 °C and pH 8, the micellar and vesicular metal catalysts show an increase of second-order rate constants (k2) by 4-7 orders of magnitude compared to the unimolecular complexes under identical conditions. At neutral pH, they produce the highest k2 values reported so far. For pBR322 plasmid DNA, both a conversion of the supercoiled to the relaxed and linear form, and also a further degradation into smaller fragments by double strand cleavages could be observed after incubation with the vesicular Zn(II)-complexes. Finally, even the cleavage of nonactivated single-stranded oligonucleotides could be considerably promoted compared to background reaction.
- Gruber, Benjamin,Kataev, Evgeny,Aschenbrenner, Jana,Stadlbauer, Stefan,Koenig, Burkhard
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- Synthesis, characterization and coordination chemistry of dibenzofuran derivatives of 1,4,7,10-tetraazacyclododecane
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A 1,4-disubstituted dibenzofuran derivative of 1,4,7,10- tetraazacyclododecane (cyclen), L1, has been prepared by the direct reaction of cyclen and chloroacetyldibenzofuran and the mono-substituted derivative, L2, by reaction of chloroacetyldibenzofuran and 1,4,7-tris(t-butoxycarbonyl)-1,4,7,10- tetraazacyclododecane followed by deprotection with trifluoroacetic acid. The ligands were characterized by 1H and 13C NMR spectroscopy, IR spectroscopy and mass spectrometry. The reaction of the 1,4-disubstituted dibenzofuran cyclen, L1, with Cu(ClO4)2·6H 2O in methanol yielded crystals of [CuL1](ClO4) 2·MeOH·1/2H2O that were suitable for single crystal structural analysis. The X-ray structure confirmed that the 1,4-disubstituted dibenzofuran cyclen had been formed. The copper(II) coordination sphere in the complex cation, [CuL1]2+, is occupied by four nitrogen atoms from the macrocycle and an amide oxygen donor from one dibenzofuran pendant group. As is typical for copper(II)-cyclen complexes, the Cu(II) centre sits above the plane of the macrocycle nitrogen towards the oxygen donor, in this case by 0.5 . Fluorescence emission studies indicate that coordination of the macrocycle to either copper(II) or zinc(II) results in a decrease in emission with respect to the emission of the pure ligand.
- Venkatachalam,Barreto, Jose,Kreher, Ute,Reutens, David C.,Spiccia, Leone
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- Coordination chemistry of a mono-dibenzofuran derivative of 1,4,7,10-tetraazacyclododecane
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Copper(II) and cadmium(II) complex of a mono-dibenzofuran derivative of 1,4,7,10-tetraazacyclododecane (cyclen), L1, have been prepared by reaction of the mono-dibenzofuran-substituted cyclen with either copper(II) or cadmium(II) perchlorate in acetonitrile. This yielded the corresponding divalent metal complexes, [Cu(L1)](ClO4)2·H2O (C1) and [Cd(L1)](ClO4)2·H2O (C2), which were isolated as single crystals suitable for X-ray crystallography by diffusing diethyl ether into an acetonitrile solution of each complex. For the copper(II) complex, C1, the X-ray crystal structure revealed a distorted square pyramidal Cu(II) coordination sphere occupied by four amine nitrogens from the cyclen ring and one oxygen from the amide linkage present in L1. On the other hand, the metal center in the cadmium complex is seven coordinate, with two weakly bound acetonitrile molecules occupying two additional coordination sites about the Cd(II) center; these bind cis to the amide oxygen. The coordination geometry is best described as monocapped trigonal prismatic. In both complexes, the secondary amine nitrogens on the cyclen macrocycle form hydrogen bonds with perchlorate counterions present in the crystal lattice. Titration of L1 with various metal ions (Mn2+, Co2+, Ni2+, Cu2+, Zn2+, and Cd2+) in acetonitrile revealed a gradual quenching of the benzofuran emission with increasing [M2+] consistent with formation of metal complexes with a 1: 1 M2+: L1 stoichiometry. From the emission data, the conditional stability constant was determined to be 10-20 times higher for the Cu(II) complex than the other divalent metal complexes investigated.
- Barreto, José,Joshi, Tanmaya,Venkatachalam,Reutens, David C.,Graham, Bim,Spiccia, Leone
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- Polymethacrylates with a covalently linked CuII-cyclen complex for the in situ generation of nitric oxide from nitrosothiols in blood
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(Figure Presented) In the matrix: A new cross-linked hydrogel polymer, poly(2-hydroxyethyl methacrylate) (pHEMA), containing appended Cu II-cyclen sites (cyclen = 1,4,7,10-tetraazacyclododecane) was prepared and shown to generate nitric oxide from endogenous S-nitrosothiol species (RSNO) typically found in circulating whole blood.
- Hwang, Sangyeul,Cha, Wansik,Meyerhoff, Mark E.
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- Cooperative self-assembly of adenosine and uridine nucleotides on a 2D synthetic template
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(Figure Presented) Double plane: Base pairing mediates sterically induced, cooperative self-assembly of complementary nucleotides on a template formed from amphiphilic bis(ZnII-cyclen) derivatives ordered on thiolated surface. Real-time monitoring of binding events proved precise harboring of equal amounts of A and U nucleotides from their arbitrary combinations in solution into planar bilayers (see picture).
- Turygin, Dmitry S.,Subat, Michael,Raitman, Oleg A.,Arslanov, Vladimir V.,Koenig, Burkhard,Kalinina, Maria A.
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- A new high-capacity metal ion-complexing gel containing cyclen ligands
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We describe a new polymeric hydrogel that binds divalent metal ions with large binding constants and capacity. A new acrylate monomer with the pendant cyclen, tri-tert-butyl-10-(2-(2-(2-(methacryloyloxy)ethoxy)ethoxy)-2-oxoethyl)-1,4,7,10-tetraazacyclododecane-1,4,7-tricarboxylate, was polymerised by RAFT to a roughly spherical 5-9 unit oligomer bearing a carboxylate-functionalised end-group. This was de-protected and coupled to an amine dendrimer then crosslinked into a nylon-type hydrogel capable of absorbing more than 10 wt% copper ions.
- Dolan, Ciarán,Drouet, Fleur,Ware, David C.,Brothers, Penelope J.,Jin, Jianyong,Brimble, Margaret A.,Williams, David E.
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- Cu(II)-Based Paramagnetic Probe to Study RNA-Protein Interactions by NMR
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Paramagnetic NMR techniques allow for studying three-dimensional structures of RNA-protein complexes. In particular, paramagnetic relaxation enhancement (PRE) data can provide valuable information about long-range distances between different structural components. For PRE NMR experiments, oligonucleotides are typically spin-labeled using nitroxide reagents. The current work describes an alternative approach involving a Cu(II) cyclen-based probe that can be covalently attached to an RNA strand in the vicinity of the protein's binding site using "click" chemistry. The approach has been applied to study binding of HIV-1 nucleocapsid protein 7 (NCp7) to a model RNA pentanucleotide, 5′-ACGCU-3′. Coordination of the paramagnetic metal to glutamic acid residue of NCp7 reduced flexibility of the probe, thus simplifying interpretation of the PRE data. NMR experiments showed attenuation of signal intensities from protein residues localized in proximity to the paramagnetic probe as the result of RNA-protein interactions. The extent of the attenuation was related to the probe's proximity allowing us to construct the protein's contact surface map.
- Seebald, Leah M.,Demott, Christopher M.,Ranganathan, Srivathsan,Asare Okai, Papa Nii,Glazunova, Anastasia,Chen, Alan,Shekhtman, Alexander,Royzen, Maksim
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- Preparation and characterization of an improved Cu2+-cyclen polyurethane material that catalyzes generation of nitric oxide from S-nitrosothiols
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A new, stable and highly efficient Cu2+-cyclen-polyurethane material is described and shown to exhibit an improved performance compared to that of prior materials for the catalytic decomposition of S-nitrosothiols to physiologically active nitric oxide. The Royal Society of Chemistry.
- Liu, Kun,Meyerhoff, Mark E.
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- Design, Synthesis, and Biological Evaluation of Boron-Containing Macrocyclic Polyamines and Their Zinc(II) Complexes for Boron Neutron Capture Therapy
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Boron neutron capture therapy (BNCT) is a binary therapeutic method for cancer treatment based on the use of a combination of a cancer-specific drug containing boron-10 (10B) and thermal neutron irradiation. For successful BNCT,10B-containing molecules need to accumulate specifically in cancer cells, because destructive effect of the generated heavy particles is limited basically to boron-containing cells. Herein, we report on the design and synthesis of boron compounds that are functionalized with 9-, 12-, and 15-membered macrocyclic polyamines and their Zn2+complexes. Their cytotoxicity, intracellular uptake activity into cancer cells and normal cells, and BNCT effect are also reported. The experimental data suggest that mono- and/or diprotonated forms of metal-free [12]aneN4- and [15]aneN5-type ligands are uptaken into cancer cells, and their complexes with intracellular metals such as Zn2+would induce cell death upon thermal neutron irradiation, possibly via interactions with DNA.
- Ueda, Hiroki,Suzuki, Minoru,Kuroda, Reiko,Tanaka, Tomohiro,Aoki, Shin
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p. 8523 - 8544
(2021/06/28)
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- DINUCLEATING LIGAND OR DINUCLEAR METAL COMPLEX
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To provide a metal complex that has high cancer cell toxicity and has DNA target and cyclen.SOLUTION: The present disclosure provides a dinuclear metal complex represented by the following formula (IV).SELECTED DRAWING: None
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Paragraph 0060-0061
(2021/03/19)
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- Catalytic Hydrolysis of Phosphate Monoester by Supramolecular Phosphatases Formed from a Monoalkylated Dizinc(II) Complex, Cyclic Diimide Units, and Copper(II) in Two-Phase Solvent System
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Design and synthesis of enzyme mimic with programmed molecular interaction among several building blocks including metal complexes and metal chelators is of intellectual and practical significance. The preparation of artificial enzymes that mimic the natu
- Rahman, Akib Bin,Imafuku, Hiroki,Miyazawa, Yuya,Kafle, Ananda,Sakai, Hideki,Saga, Yutaka,Aoki, Shin
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p. 5603 - 5616
(2019/05/01)
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- PET bone imaging agent precursor and synthesis method thereof
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The invention discloses a PET bone imaging agent precursor, wherein a linking agent tripolyethanol is introduced between a macrocyclic polyamine ligand and a targeting carrier diphosphonic acid, and the diphosphonic acid bone-seeking group with targeting effect can form the macrocyclic polyamine cooperation group of a stable chelate with a plurality of metal nuclides so as to form a bone imaging agent. According to the present invention, the synthesized precursor compound contains the bone-seeking group (diphosphonic acid) and the cooperation group (DOTA), and the two functional groups are linked by PFG3, such that the precursor compound has remarkable structural characteristics; the precursor compound has strong bone-seeking property, and can form a complex (marker) with kinetic and thermodynamic stability with metal nuclides; the marker formed by marking the precursor with different metal nuclides can be used as a bone imaging agent (marked with Cu, Ga and other positron emission metal nuclides) with powerful functions, and can further be used as an ideal bone tumor treatment drug (marked with In, Y, Zr, Sm and other radioactive treatment metal nuclides).
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Paragraph 0059
(2019/12/10)
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- Preparation method of gadavist intermediate
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The invention relates to a preparation method of a gadavist intermediate GDB1. According to the preparation method, cycleanine is used as a starting material, Boc anhydride is used for protecting three amino groups, then the cycleanine is subjected to a reaction with 4,4-dimethyl-3,5,8-trioxabicyclooctane[5.1.0], hydrochloric acid is added for hydrolysis after the completion of the reaction, and the GDB1 with relatively high purity and good yield is obtained.
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Paragraph 0031-0033
(2018/12/13)
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- Novel tinib-type compound, preparation method and application thereof
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The invention provides a novel tinib-type compound shown as a structural formula (I), wherein R1 is selected from aryl or ceteroary the aryl or ceteroary is substituted by one or more of alkyl, halogen, aryl, alkynyl, cyano, trifluoromethyl, methoxy and halogenated benzyl; R2 is 1,4,7,10-tetraazacyclododecane or 1,4,7-triazacyclononane. The invention also provides application of the compound in preparation of antitumor medicines. The novel tinib-type compound has an obvious inhibiting effect for A549 cell lines, apoptosis of A549 cells can be obviously enhanced, and the effect is obviously superior to that of gefitinib. (The structural formula is shown in the specification).
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Paragraph 0041; 0051; 0052
(2018/07/03)
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- BINUCLEATING LIGAND OR BINUCLEAR METAL COMPLEX
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PROBLEM TO BE SOLVED: To provide a binuclear metal complex that can be easily synthesized and has a proper anticancer action. SOLUTION: The present invention provides a binuclear metal complex represented by the following chemical formula (IV). SELECTED DRAWING: Figure 1 COPYRIGHT: (C)2018,JPOandINPIT
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Paragraph 0041; 0042
(2018/09/25)
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- Amphiphilic Tb (III) complex and method of preparing the same and of spiral fluorescent nano fiber preparation method and application
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The invention discloses an amphiphilic Tb(III) complex and a preparation method thereof and a preparation method and use of spiral fluorescent nanofiber, an amphiphilic molecule with cholesterol molecules a hydrophobic tail part and a lanthanide metal complex as a hydrophilic head group is prepared, by use of strong cholesterol molecular self-assembly characteristics, the spiral fluorescent nanofiber is assembled in aqueous phase, the fluorescent nanofiber not only has the characteristics of long fluorescence lifetime, narrow emission spectral band, large stoke shift and the like of lanthanide metals, and also has the characteristics of large receptor molecule local concentration, strong pre-organization ability, adjustable interface local conformation and the like. Through use of collaborative complexation between receptor molecules and substrate molecules assembled at the interface and energy transfer process, high sensitive different conformation differentiation of oligonucleotide can be realized, and efficient detection of K + can be realized.
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Paragraph 0061-0063
(2017/02/28)
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- UBA5 INHIBITORS
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The present disclosure relates to compounds of the Formula (I), which are UBA5 inhibitors.
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Paragraph 00107; 00108; 00109
(2015/12/18)
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- ANTIBACTERIAL COMPOUNDS
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The invention relates to antibacterial compounds, methods for synthesis and use thereof in antibacterial applications.
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Page/Page column 42; 43
(2014/10/15)
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- Non-covalent immobilization of rare earth heterobimetallic frameworks and their reactivity in an asymmetric Michael addition
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Heterobimetallic Lewis acid catalysts are broadly useful and methods to recycle them have immediate applications. However, their immobilization through covalent binding can be challenging. Non-covalent immobilization of supported asymmetric catalysts is attractive due to ease of preparation and potential for reversible binding. We report a novel non-covalent binding strategy for Shibasaki's REMB framework {RE=rare earth metal; M=Li, Na, K; B=BINOL; RE:M:B=1:3:3, [M3(sol)n][(BINOLate)3RE]} and explore the reactivity of the supported catalyst.
- Robinson, Jerome R.,Yadav, Jagjit,Fan, Xinyuan,Stanton, Gretchen R.,Schelter, Eric J.,Pericas, Miquel A.,Walsh, Patrick J.
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p. 1243 - 1254
(2014/05/06)
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- Synthesis and characterization of binuclear Zn(II)-cyclen complexes bridged by α,ω-bis(4-methylphenoxy) alkanes
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A series of novel α,ω-bis(4-methylphenoxy) alkane functionalized cyclen ligands were synthesized by the nucleophilic substitution reaction of 1,4,7-tris(tert-butyloxycarbonyl)-1,4,7,10-tetraazacyclododecane and α,ω-bis(4-bromomethylphenoxy) alkanes. The corresponding dimeric Zn(II)-cyclen complexes were obtained by reaction of these ligands with Zn(ClO4)2·6H2O. Ligands and complexes were characterized by FT-IR, 1H NMR, and elemental analysis. Springer Science+Business Media B.V. 2012.
- Wan, Fuxian,Li, Changcheng,Jiang, Lin,Li, Ying
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p. 2085 - 2096
(2013/02/23)
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- Modular 'click' sensors for zinc and their application in vivo
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Although the central role that zinc plays in many biological processes and important disease states is now well-established, there remains a pressing need to develop an absolute understanding of the underlying biology of zinc trafficking in terms of its dynamic and quantitative processing in specific organelles. Here we describe the modular synthesis of zinc sensors using a 'click' approach and demonstrate the applicability of our new sensors in vivo using a zebrafish model.
- Jobe, Kajally,Brennan, Caroline H.,Motevalli, Majid,Goldup, Stephen M.,Watkinson, Michael
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supporting information; experimental part
p. 6036 - 6038
(2011/08/02)
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- Fluorescent bis-cyclen tweezer receptors for inositol (1,4,5)-trisphosphate
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Herein, we report the development of two fluorescent sensors for inositol 1,4,5-trisphosphate (InsP3), containing either two free cyclen or zinc(II)/cyclen groups preorganized into a binding cleft. Preorganization was achieved using a rigid acr
- Do-Thanh, Chi-Linh,Rowland, Meng M.,Best, Michael D.
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experimental part
p. 3803 - 3808
(2011/06/21)
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- Zinc(II)cyclen-peptide conjugates interacting with the weak effector binding state of Ras
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Zinc(II)cyclen-peptide hybrid compounds and bis-zinc(II)cyclen complexes are prepared as potential binders of the guanine nucleotide binding protein Ras, an important molecular switch in cellular signal transduction. The design of the compounds is based on the previous observation that zinc(II)cyclen complexes could serve as lead compounds for inhibitors of Ras-effector interaction and thus be able to interrupt Ras induced signal transduction. Zinc(II)cyclen selectively stabilizes conformational state 1 of active Ras, a conformational state with drastically decreased affinity to effector proteins like Raf-kinase. To achieve higher binding affinities of such Ras-Raf interaction inhibitors, zinc(II)cyclen conjugates with short peptides, derived from the sequence of the Ras-activator SOS, were prepared by solid phase synthesis protocols. Dinuclear bis-zinc(II)cyclen complexes were obtained from alkyne-azide cycloaddition reactions. NMR investigations of the prepared compounds revealed that the peptide conjugates do not lead to an increase in Ras binding affinity of the metal complex-peptide conjugates. The dinuclear zinc complexes lead to an immediate precipitation of the protein prohibiting spectroscopic investigations of their binding.
- Schmidt, Florian,Rosnizeck, Ina C.,Spoerner, Michael,Kalbitzer, Hans Robert,K?nig, Burkhard
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scheme or table
p. 38 - 48
(2011/03/22)
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- Binuclear terbium(III) complex as a probe for tyrosine phosphorylation
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By using the luminescence from binuclear complexes of TbIII (Tb2L1 and Tb2-L2), phosphorylated Tyr residue in peptides was selectively detected in neutral aqueous solutions. Neither the non-phosphorylated Tyr, pSer, pThr, nor the other phosphate-containing biomolecules tested affected the luminescence intensity to any notable extent. Upon the binding of the pTyr to these TbIII complexes, the luminescence from the metal ion was notably promoted, as the light energy absorbed by the benzene ring of pTyr is efficiently transferred to the TbIIIcenter. The binding activity of the binuclear Tb III complexes towards pTyr is two orders of magnitude larger than that of the corresponding mononuclear complex. These binuclear complexes were successfully used for real-time monitoring of enzymatic phosphorylation of a peptide by a tyrosine kinase.
- Akiba, Hiroki,Sumaoka, Jun,Komiyama, Makoto
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supporting information; experimental part
p. 5018 - 5025
(2010/09/03)
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- PYRIDYL-AZA(THIO)XANTHONE SENSITIZER COMPRISING LANTHANIDE(III) ION COMPLEXING COMPOUNDS, THEIR LUMINESCENT LANTHANIDE (III) ION COMPLEXES AND USE THEREOF AS FLUORESCENT LABELS.
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Lanthanide (III) Ion completing compound comprising: (1) a sensitizer moiety of Formula (I) in which: a is an integer from 1 to 4; b is an integer equal to 1 or 2; c is an integer equal to 1 or 2; (R1)a, (R2)b, (R3)C are t
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Page/Page column 43; 44
(2010/08/08)
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- Artificial transcription factors which mediate double-strand DNA Cleavage
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A new family of artificial transcription factor (ATF)-based conjugates have been designed and synthesized as potent chemical nucleases. Polyamides as the important and efficient ATFs were used to modify and activate several anchor compounds. The results demonstrate that the resulting conjugates remarkably promote the rate accelerations and non-random double-strnd DNA cleavage activity. Interestingly, the cleavage activity of both the hydrolytic and oxidative agents was promoted efficiently through the modification of the ATFs.
- Li, Chao,Du, Chao,Tian, Hua,Jiang, Chao,Du, Min,Liu, Yan,Qiao, Ren-Zhong,Jia, Yan-Xing,Zhao, Yu-Fen
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supporting information; scheme or table
p. 12935 - 12940
(2011/02/25)
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- Zn2+ cation triggers self-assembly of cyclen into a stable metallogel
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A novel type of ligands contained 1,4,7,10-tetrazacyclododecane and functionalized by two azobenzene moieties grafted with two alkyl chains was designed and synthesized. The ligands with long alkyl chains can form metallogels in the presence of Zn2+ cations. The formation of metallogel was followed by NMR and electronic spectral detection. The morphology of the xerogels is varied with the equivalent of Zn2+ cations and the concentration of the gel. Spectral and structural analysis indicated that the driving forces of the gel formation were attributed to intermolecular hydrophobic interactions between alkyl chains and π-π interaction between azobenzenes.
- Shu, Tianmin,Wu, Junchen,Zou, Ying,Liu, Keyin,Chen, Liqing,Yi, Tao
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scheme or table
p. 184 - 192
(2011/11/29)
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- LANTHANIDE (III) ION COMPLEXING COMPOUNDS, LUMINESCENT LANTHANIDE (III) ION COMPLEXES AND USE THEREOF AS FLUORESCENT LABELS
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Lanthanide (III) ion complexing compound comprising: (1) a sensitizer moiety of formula (I) in which: a is an integer from 1 to 4; b is an integer equal 1 or 2; c is an integer equal to 1 or 2; (R1)a, (R2)b, (R3)C are the
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Page/Page column 23; 30-31
(2009/03/07)
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- The effect of an amino-acid bridge on binding affinity and cleavage efficiency of pyrenyl-macrocyclic polyamine conjugates toward DNA
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A series of pyrenyl-macrocyclic polyamines 5a-5c have been prepared and characterized. Their DNA-cleavage properties were examined under physiological conditions. Without the presence of other additives, the DNA cleavage ability of 5a -5c showed the order
- Lu, Qiao-Sen,Huang, Yu,Li, Jing,Zhang, Zhong-Wei,Lin, Hong-Hui,Yu, Xiao-Qi
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scheme or table
p. 1273 - 1282
(2010/04/23)
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- Responsive Mri Contrast Agents
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The invention provides MRI contrast agents which provide a high sensitivity and which have an optimised body retention time. These agents enable the mapping of the local pH, temperature, oxygen concentration or other metabolites in a patient's body by the
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Page/Page column 4-5
(2008/12/07)
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- Tripodal, cooperative, and allosteric transphosphorylation metallocatalysts
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Three artificial amino acids derived from L-serine by replacing the hydroxyl moiety with 1,4,7-triazacyclononane, 1,5,9-triazacyclododecane, and 1,4,7,10-tetraazacyclododecane, respectively, have been connected to the three arms of the tetraamine tris(2-a
- Scarso, Alessandro,Zaupa, Giovanni,Houillon, Florence Bodar,Prins, Leonard J.,Scrimin, Paolo
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p. 376 - 385
(2007/10/03)
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- Highly regioselective N-trans symmetrical diprotection of cyclen
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A high yielding N-trans diprotection procedure for cyclen has been developed by using succinimide carbamate derivates of Boc and Cbz and chloroformate protecting groups.
- De León-Rodríguez, Luis M.,Kovacs, Zoltan,Esqueda-Oliva, Ana Cristina,Miranda-Olvera, Alma Delia
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p. 6937 - 6940
(2007/10/03)
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- Synthesis and binding properties of hybrid cyclophane - Azamacrocyclic receptors
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(Chemical Equation Presented). Three new azamacrocyclic-cyclophane hybrid receptors L1, L2, and L3 have been synthesized that incorporate either 1,4,7,10-tetraazacyclododecane (cyclen) or 1,4,7-triazacyclononane (tacn) uni
- Benniston, Andrew C.,Gunning, Patrick,Peacock, Robert D.
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p. 115 - 123
(2007/10/03)
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- Synthesis, relaxometric and photophysical properties of a new pH-responsive MRI contrast agent: The effect of other ligating groups on dissociation of a p-nitrophenolic pendant arm
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Two gadolinium(III) chelates, GdNP-DO3A (1-methlyene-(p-NitroPhenol)-1,4,7, 10-tetraazacycloDOdecane-4,7,10-triAcetate) and GdNP-DO3AM (1-methlyene(p- NitroPhenol)-1,4,7,10-tetraazacycloDOdecane-4,7,10-triacetAMide), containing a single nitrophenolic pendant arm plus either three acetate or three amide pendant arms were synthesized and characterized. The properties of the gadolinium, terbium, and dysprosium complexes of these ligands were examined as a function of pH. The extent and mechanism of the changes in water relaxivity with pH of each gadolinium complex was found to differ substantially for the two complexes. The water relaxivity of Gd(NP-DO3A) increases from 4.1 mM -1 s-1 at pH 9 to 7.0 mM-1 s-1 at pH 5 as a result of acid-catalyzed dissociation of the nitrophenol from the lanthanide. The nitrophenol group in Gd(NP-DO3AM) does not dissociate from the metal center even at pH 5; therefore, the very modest increase in relaxivity in this complex must be ascribed to an increase in prototropic exchange rate of the bound water and/or phenolic protons.
- Woods, Mark,Kiefer, Garry E.,Bott, Simon,Castillo-Muzquiz, Aminta,Eshelbrenner, Carrie,Michaudet, Lydie,McMillan, Kenneth,Mudigunda, Siva D. K.,Ogrin, Doug,Tircso, Gyula,Zhang, Shanrong,Zhao, Piyu,Sherry, A. Dean
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p. 9248 - 9256
(2007/10/03)
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- Solid-Phase Assisted N-1 Functionalization of Azamacrocycles
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A simple solid-phase assisted strategy for the N-1 functionalization of azamacrocycles is described. Compounds such as cyclen, cyclam and piperazine can be selectively modified by temporary attachment to solid-phase resins providing an efficient and clean method to prepare biomedically interesting moieteies.
- Oliver, Morag,Jorgensen, Michael R.,Miller, Andrew D.
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p. 453 - 456
(2007/10/03)
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- Synthesis of an amino acid with protected cyclen side chain functionality
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Starting from glutamic acid an artificial amino acid with 1,4,7,10-tetraazacyclododecane (cyclen) side chain functionality is prepared. The orthogonal protected building block allows the facile introduction of a metal ion binding site into peptide structu
- Miltschitzky, Stefan,Koenig, Burkhard
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p. 2077 - 2084
(2007/10/03)
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- A tris(Zn(II)-1,4,7,10-tetraazacyclododecane) complex as a new receptor for phosphate dianions in aqueous solution
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A new tris(Zn(II)-cyclen) (Zn3L3), which has three Zn(II)-macrocyclic tetraamine (cyclen) complexes connected through a 1,3,5-trimethylbenzene spacer, has been synthesized as a novel receptor for organic phosphate dianions in aqueous solution (cyclen = 1,4,7,10-tetraazacyclododecane and L3 = 1,3,5-tris(1,4,7,10-tetraazacyclododecan-1-ylmethyl)benzene). The design of Zn3L3 was based on X-ray crystal structure analysis of the 1:3 complex of 4-nitrophenyl phosphate (NPP2-) with Zn(II)-cyclen (ZnL1) complex. The potentiometric pH titration of Zn3L3.3H2O revealed the deprotonation constants of the three Zn(II)-bound H2O molecules to be 6.1 (pK1), 7.3 (pK2), and 8.6 (pK3) at 25 °C with I = 0.1 (NaNO3). These three stepwise deprotonations and 1H NMR spectra changes at various pD values in D2O suggest that strong intramolecular hydrogen bonds link each adjacent Zn(II)-OH2 (or Zn(II)-OH-) at neutral pH in aqueous solution. At higher pH (> 9), the hydrogen bond network disrupts. The 31P NMR titration of Zn3L3.3H2O with phenyl phosphate dianion (PP2-) in D2O confirmed the formation of a 1:1 complex (Zn3L3-PP2-). By potentiometric pH titrations, the 1:1 complex affinity constants, log K(aff) (K(aff) = [phosphate complex]/[Zn(II) complex] [phosphate] (M-1)), were determined to be 5.8 with NPP2-, 6.6 with PP2-, 7.0 with α-D-glucose-1-phosphate, and 7.9 with phenyl phosphonate in aqueous solution. The tris(Zn(II)-cyclen) complex is found to be a much better host toward phosphates than the parent Zn(II)-cyclen (ZnL1) (log K(aff) = 3.3 for ZnL1-NPP2-) or a bis(Zn(II)-cyclen) linked with a m-xylene spacer (Zn2L2) (log K(aff) = 4.0 for Zn2L2-NPP2-).
- Kimura, Eiichi,Aoki, Shin,Koike, Tohru,Shiro, Motoo
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p. 3068 - 3076
(2007/10/03)
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- New facile and convenient synthesis of bispolyazamacrocycles using Boc protection. Determination of geometric parameters of dinuclear copper(II) complexes using ESR spectroscopy and molecular mechanics calculations
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A new facile and convenient synthetic route has been designed for the preparation of bispolyazamacrocycles in high yields by direct condensation of the readily available intermediate //,W-diboctriazamacrocycle or N,N',N"triboctetraazamacrocycles with aromatic biselectrophiles, ie, o-, m-, p-xylyl and anthracenyl derivatives. The use of a versatile group, such as ferf-butyloxycarbonyl (Boc), which is easily removed within l h by treatment with 6 M HC1 or TFA, leads to polyazamacrocycles in which one nitrogen is discriminated from the others. The anthracenyl and o-xylyl dimers were synthesized by reacting diacyl chloride to give the corresponding diamides. Further reduction of the amide groups and elimination of the protecting Boc moieties were carried in a one-pot reaction with BHa-THF followed by acid treatment. In parallel, exclusive mono-JV-alkylation of the available secondary amine of the same protected macrocycle with the corresponding dibromoxylene gave the meta and para dimers; the protecting moieties were eliminated in a similar way. ESR measurements of spin-spin distances of the dicopper complexes were determined from the ratio of the intensity of the forbidden transition to the intensity of the allowed transitions. Molecular mechanics calculations were also undertaken in order to evaluate the Cu-Cu distance by using a new rule-based force field. Eisevier,.
- Brandes, Stephane
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