Search results for "ligands"

showing 10 items of 721 documents

Structure of SNX9 SH3 in complex with a viral ligand reveals the molecular basis of its unique specificity for alanine-containing class I SH3 motifs

2021

Class I SH3 domain-binding motifs generally comply with the consensus sequence [R/K]x0PxxP, the hydrophobic residue 0 being proline or leucine. We have studied the unusual 0 = Ala-specificity of SNX9 SH3 by determining its complex structure with a peptide present in eastern equine encephalitis virus (EEEV) nsP3. The structure revealed the length and composition of the n-Src loop as important factors determining specificity. We also compared the affinities of EEEV nsP3 peptide, its mutants, and cellular ligands to SNX9 SH3. These data suggest that nsP3 has evolved to minimize reduction of conformational entropy upon binding, hence acquiring stronger affinity, enabling takeover of SNX9. The R…

DYNAMICSPROLINE-RICH PEPTIDESviruksetPROTEINSvirusesHTLV-1 GagLigandsEVOLUTIONARY CONSERVATIONalfaviruksetsrc Homology DomainsHIGH-AFFINITYretroviruksetDOMAINStructural BiologyBINDINGAnimalsHorsesMolecular Biologysoluviestintä11832 Microbiology and virologyAlanineBinding SitesPXXP MOTIFSisothermal titration calorimetrySH3solution NMR spectroscopyEEEV nsP3HIV-11182 Biochemistry cell and molecular biologyproteiinitCHEMICAL-SHIFTS3111 BiomedicinePeptidesSNX9Protein Binding
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Ligand-based discovery of novel trypanosomicidal drug-like compounds: In silico identification and experimental support

2010

Abstract Two-dimensional bond-based linear indices and linear discriminant analysis are used in this report to perform a quantitative structure–activity relationship study to identify new trypanosomicidal compounds. A database with 143 anti-trypanosomal and 297 compounds having other clinical uses, are utilized to develop the theoretical models. The best discriminant models computed using bond-based linear indices provides accuracies greater than 90 for both training and test sets. Our models identify as anti-trypanosomals five out of nine compounds of a set of already-synthesized substances. The in vitro anti-trypanosomal activity of this set against epimastigote forms of Trypanosoma cruzi…

Databases FactualMolecular modelCell SurvivalStereochemistryTrypanosoma cruziIn silicoNitro compoundQuantitative Structure-Activity RelationshipComputational biologyLigandsChemometricsDrug DiscoveryAnimalsHumansChagas DiseaseTrypanosoma cruziAmastigotePharmacologychemistry.chemical_classificationLife Cycle StagesbiologyOrganic ChemistryDiscriminant AnalysisBiological activityGeneral MedicineFibroblastsModels Theoreticalbiology.organism_classificationLinear discriminant analysisTrypanocidal AgentsHigh-Throughput Screening AssayschemistryAlgorithmsSoftwareEuropean Journal of Medicinal Chemistry
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Ruthenium Metallodendrimers Based on Nitrile‐Functionalized Poly(alkylidene imine)s

2005

The preparation of the first- and second-generation of nitrile-functionalized poly(alkylidene imine) dendrimers with the organometallic ruthenium complex [Ru(η5-C5H5)(PPh3)2Cl] peripherally attached is described. The reaction of N,N′-bis(cyanomethyl)piperazine (1), N,N′-bis[N′′,N′′′-bis(cyanoethyl)aminoethyl]piperazine (2), or N,N,N′,N′-tetrakis(cyanoethyl)ethylenediamine (3) with [Ru(η5-C5H5)(PPh3)2Cl] (4) in the presence of TlPF6 gives the new air-stable ruthenium metallodendrimers 5, 6, and 7, respectively. These stable metallodendrimers are easily prepared and represent a novel quantitative method to solidify and chromatographically purify the otherwise semi-liquid nitrile-functionalize…

DendrimersNitrileIminechemistry.chemical_elementEthylenediamineSandwich complexes.Mass spectrometryRutheniumRutheniumInorganic ChemistryFaculdade de Ciências Exatas e da Engenhariachemistry.chemical_compoundPiperazineN ligandschemistryDendrimerPolymer chemistryOrganic chemistry31p nmr spectroscopyEuropean Journal of Inorganic Chemistry
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Preparation and Characterization of Novel Poly(alkylidenamine) Nitrile Ruthenium Metallodendrimers

2010

Complete functionalization of N,N,N',N'-[tetrakis(cyanoethyl)-hexamethylenediamine] [N≡C(CH 2 ) 2 ] 2 N(CH 2 ) 6 N[(CH 2 ) 2 -C≡N] 2 (4) and N,N,N',N'-(tetrakis(cyanoethoxypropyl)hexamethylenediamine] [N≡C(CH 2 ) 2 O(CH 2 ) 3 ] 2 N(CH 2 ) 6 N[(CH 2 ) 3 -O(CH 2 ) 2 C≡N] 2 (7) with the organometallic moiety [Ru(η 5 -C 5 H 5 )(PPh 3 ) 2 Cl] and the five-coordinate cis-[RuCl(dppe) 2 ]-[PF 6 ] [dppe = 1,2-bis(diphenylphosphanyl)ethane] was attained with good yield, respectively, by treating the metallo-fragment with the core in methanol (at room temperature and in presence of TIPF 6 as a chloride abstractor) and in 1,2-dichloroethane (under reflux). These novel nitrile-functionalized poly(alkyli…

DendrimersPolynuclear complexesNitrileStereochemistrychemistry.chemical_elementMetallodendrimerSandwich complexes.Medicinal chemistryRutheniumRutheniumInorganic ChemistryFaculdade de Ciências Exatas e da Engenhariachemistry.chemical_compoundN ligandschemistryHexamethylenediamineDendrimerYield (chemistry)MoietyMethanolEuropean Journal of Inorganic Chemistry
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New insights into the reactivity of the tantalocene hydride Cp′2TaH3 (Cp′=η5-tBuC5H4). Synthesis and characterisation of cationic Ta(V) complexes wit…

2002

Abstract Reaction of various neutral LXH bidentate ligands (2-aminobenzoic acid, acetylacetone, dibenzoylmethan and 2-aminobenzenethiol) with [Cp′2TaH2]+, obtained in situ from Cp′2TaH3 treated with triphenylmethan cation, affords after dihydrogen elimination the corresponding cationic species [Cp′2Ta(H)(LX)]+ in BF4 or PF6 salts. Complexes [Cp′2TaH(η2-O2CC6H4-o-NH2O,O′)]PF6 (3), {Cp′2Ta[η2-OC(Me)CHC(Me)OO,O′]}BF4 (4a), {Cp′2TaH[η2-OC(Ph)CHC(Ph)OO,O′]}BF4 (4b) and [Cp′2TaH(η2-SC6H4-o-NH2S,N)]PF6 (5) are characterised by analytical and spectroscopic methods. With thiopyridine, the kinetic (6) and the thermodynamic (6′) isomers [Cp′2TaH(η2-2-SC5H4NS,N)]PF6 are identified. Crystal struc…

DenticityChelating ligandsStereochemistryHydrideAcetylacetoneOrganic ChemistryCationic polymerizationCrystal structureBiochemistryMedicinal chemistryInorganic Chemistrychemistry.chemical_compoundchemistryMaterials ChemistryReactivity (chemistry)Physical and Theoretical ChemistryJournal of Organometallic Chemistry
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Acetazolamide-M(II) [M(II) = Co(II), Ni(II), Cu(II)] complexes with ethylamine, diethylamine, triethylamine, and potassium hidroxide

1991

Abstract Complexes of Co(II), Ni(II), and Cu(II) with dideprotonated Acm are synthesized and characterized. Acm acts as bidentate ligand through the N-sulfonamido atom and the N-thiadiazole atom except for K6CoAcm4·6H2O in which Acm behaves as monodentate through the N-sulfonamido atom.

DenticityDiethylaminesPotassium CompoundsPotassiumInorganic chemistrychemistry.chemical_elementLigandsBiochemistryMedicinal chemistryInorganic Chemistrychemistry.chemical_compoundNickelEthylaminesHydroxidesmedicineTriethylamineDiethylamineChemistrySpectrophotometry AtomicCobaltAcetazolamideSpectrophotometryPotassiumEthylamineAcetazolamideCoppermedicine.drugJournal of Inorganic Biochemistry
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Dynamic chemical devices: photoinduced electron transfer and its ion-triggered switching in nanomechanical butterfly-type bis(porphyrin)terpyridines.

2005

A series of butterfly-type molecular constructs has been prepared in good yield by using a double Stille coupling synthetic protocol. They are composed of a terpyridine (terpy) scaffold and two wings composed of appended porphyrins that are capable of switching from an extended W geometry to a compact U geometry upon cation coordination of the terpy unit. The porphyrin moieties exist in the constructs either as free bases or they can be sequentially metallated, thus giving rise to wings of different "colours". Stationary and time-resolved emission studies of the HZn, ZnAu and Zn2Au constructs show that the electronic properties are strongly dependent on the geometry. In the extended W confo…

DenticityMagnetic Resonance SpectroscopyPorphyrinsChemical PhenomenaPhotochemistryPyridinesMolecular ConformationElectronsPhotochemistryCrystallography X-RayLigandsCatalysisPhotoinduced electron transferchemistry.chemical_compoundElectron transferLigandHydrogen bondChemistry PhysicalOrganic ChemistryTemperatureGeneral ChemistryHydrogen-Ion ConcentrationPorphyrinZincSpectrometry FluorescencechemistryExcited stateSpectrometry Mass Matrix-Assisted Laser Desorption-IonizationIndicators and ReagentsSpectrophotometry UltravioletTerpyridineChemistry (Weinheim an der Bergstrasse, Germany)
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Synthetic, structural and biochemical studies of polynuclear platinum(II) complexes with heterocyclic ligands.

2008

"Non-classical" di- and trinuclear Pt(II) complexes with polydentate nitrogen ligands; ionic [(PtCl(2))(2)(tptz)(2)(mu-PtClNCPh)]Cl (1) [tptz =2,4,6-tris(2-pyridyl)-1,3,5-triazine], [(PtCl(2))(2)(bptz)(2)(mu-Pt)]Cl(2) (2) [bptz = 3,6-bis(2-pyridyl)-1,2,4,5-tetrazine] and neutral [(PtCl(2))(2)(tptz)(2)(mu-PtCl(2))](H(2)O)(4) (3), [(PtCl(2))(2)(mu-tppz)](CHCl(3)) (4) [tppz = 2,3,5,6-tetra(2-pyridyl)pyrazine] complexes, have been prepared and structurally characterized. The neutral tptz and tppz complexes present three and two separate PtCl(2) moieties, respectively, in a cis position, presumably acting in a bifunctional mode towards DNA; the cationic tptz and bptz complexes contain monofuncti…

DenticityMagnetic Resonance SpectroscopyPyrazineSpectrophotometry InfraredStereochemistryCell SurvivalCytotoxicitychemistry.chemical_elementPlatinum CompoundsLigandsChemical synthesisPolydentate nitrogen ligandchemistry.chemical_compoundHeterocyclic CompoundsCell Line TumorDrug DiscoveryHumansBifunctionalPharmacologyMolecular StructureLigandOrganic ChemistryCationic polymerizationBiological activityGeneral MedicinechemistryPolynuclear platinum complexeSettore CHIM/03 - Chimica Generale E InorganicaPlatinumEuropean journal of medicinal chemistry
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High-dimensional mixed-valence copper cyanide complexes: Syntheses, structural characterizations and magnetism

2009

International audience; Reactions of CuCl 2 with different CN complexes in presence of a neutral ancillary ligand lead to two novel mixed-valence Cu complexes [Cu II (bpy)Cu I (CN) 3 ] n , 1 (bpy=2,2′-bipyridine) and {[Cu II (tn) 2 ][Cu I 4 (CN) 6 ]} n 2 (tn=1,3-diaminopropane). For compound 1, the asymmetric unit involves two Cu ions Cu1 and Cu2 (Cu I and Cu II centres, respectively) which strongly differ in their environments. The Cu1 ion presents a CuC 4 pseudo-tetrahedral geometry, while the Cu2 ion presents a CuN 5 slightly distorted square-pyramidal geometry. The extended structure of 1 is generated by three cyano ligands which differ in their coordination modes. One CN group has a μ …

DenticityMagnetismInorganic chemistrychemistry.chemical_element[CHIM.INOR]Chemical Sciences/Inorganic chemistry010402 general chemistry01 natural sciencesCoordination modesIonInorganic ChemistryParamagnetismMagnetic propertiesMaterials ChemistryMixed-valence[CHIM.COOR]Chemical Sciences/Coordination chemistryPhysical and Theoretical ChemistryValence (chemistry)Bridging ligands010405 organic chemistryLigand[CHIM.ORGA]Chemical Sciences/Organic chemistryCopper0104 chemical sciencesCrystallographyCopper cyanideschemistryCN-group
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Mono- and Binuclear Copper(II) and Nickel(II) Complexes with the 3,6-Bis(picolylamino)-1,2,4,5-Tetrazine Ligand

2021

Four new compounds of formulas [Cu(hfac)2(L)] (1), [Ni(hfac)2(L)] (2), [{Cu(hfac)2}2(µ-L)]·2CH3OH (3) and [{Ni(hfac)2}2(µ-L)]·2CH3CN (4) [Hhfac = hexafluoroacetylacetone and L = 3,6-bis(picolylamino)-1,2,4,5-tetrazine] have been prepared and their structures determined by X-ray diffraction on single crystals. Compounds 1 and 2 are isostructural mononuclear complexes where the metal ions [copper(II) (1) and nickel(II) (2)] are six-coordinated in distorted octahedral MN2O4 surroundings which are built by two bidentate hfac ligands plus another bidentate L molecule. This last ligand coordinates to the metal ions through the nitrogen atoms of the picolylamine fragment. Compounds 3 and 4 are cen…

DenticityMaterials science42Pharmaceutical Sciencechemistry.chemical_element5-tetrazinecrystal structure determination010402 general chemistry01 natural sciencesO.ArticleAnalytical ChemistryM.lcsh:QD241-441Julvechemistry.chemical_compoundTetrazinenickelStetsiukN 1lcsh:Organic chemistryA.Drug DiscoveryLloret[CHIM]Chemical SciencesPhysical and Theoretical ChemistryIsostructural1245-tetrazine010405 organic chemistryLigandHexafluoroacetylacetoneOrganic ChemistryMagnetic susceptibility0104 chemical sciencesNickelCrystallographyAvarvarichemistryChemistry (miscellaneous)F.Intramolecular forcecopperMolecular Medicinemagnetic propertiesnitrogen ligandsEl-Ghayoury
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