Search results for " LIGANDS"

showing 10 items of 196 documents

Suitability ofMMGBSAfor the selection of correct ligand binding modes from docking results

2018

The estimation of the correct binding mode and affinity of a ligand into a target protein using computational methods is challenging. However, docking can introduce poses from which the correct binding mode could be identified using other methods. Here, we analyzed the reliability of binding energy estimation using the molecular mechanics-generalized Born surface area (MMGBSA) method without and with energy minimization to identify the likely ligand binding modes within docking results. MMGBSA workflow (a) outperformed docking in recognizing the correct binding modes of androgen receptor ligands and (b) improved the correlation coefficient of computational and experimental results of rescor…

Molecular modelBinding energyta3111LigandsEnergy minimization01 natural sciencesBiochemistrylääkesuunnitteluSubstrate SpecificityCytochrome P-450 CYP2A6Free energy perturbationCoumarinsDrug DiscoveryHumansta317PharmacologyBinding Sitesmolecular modeling010405 organic chemistryChemistryDrug discoveryOrganic Chemistryta1182liganditreceptor and ligandslaskennallinen kemiaLigand (biochemistry)Protein Structure Tertiary0104 chemical sciencesMolecular Docking Simulation010404 medicinal & biomolecular chemistryDocking (molecular)structure based drug-designThermodynamicsMolecular MedicineproteiinitTarget proteinBiological systemProtein BindingChemical Biology & Drug Design
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Diene-Containing Half-Sandwich MoIII Complexes as Ethylene Polymerization Catalysts: Experimental and Theoretical Studies

2001

International audience; Seventeen-electron compounds of Mo III having the general formula [(h 5-C 5 R 5)Mo(h 4-diene)X 2 ] (R H, Me; diene butadiene, iso-prene, or 2,3-dimethylbutadiene; X Cl, CH 3) are a new class of ethylene polymerization catalysts. The polyethy-lene obtained shows a bimodal distribution , the major weight fraction being characterized by very long (M around 10 6) and highly linear polymer chains. The newly prepared pentamethylcyclo-pentadienyl (Cp*) derivatives are more active than the cyclopentadienyl (Cp) derivatives, but much less active than previously investigated niobium III compounds having the same stoichiometry. On the other hand, the turnover frequency of the a…

MolybdenumAgostic interactionEthylene polymerizationChain propagationbiologyChemistryNiobiumOrganic ChemistryActive site[CHIM.CATA]Chemical Sciences/CatalysisGeneral ChemistryPhotochemistryHeterolysisCatalysisDensity functional calculationsCrystallography[CHIM.POLY]Chemical Sciences/PolymersCyclopentadienyl complexPolymerizationbiology.protein[CHIM.COOR]Chemical Sciences/Coordination chemistryDensity functional theoryMulliken population analysisCyclopentadienyl ligandsChemistry - A European Journal
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Cyclopentadienylmolybdenum(VI) and molybdenum(V) oxo chemistry: New synthetic and structural features

2002

International audience; Convenient syntheses for Cp, Cp*, and related cyclopentadienyl derivatives (4Cp = C5HiPr4; Cp′′′ = C5H2tBu3-1,2,4) of formula [(Ring)2Mo2O5] are described. Compound [Cp2Mo2O5] was produced in good yields by the rapid oxidation of red [CpMoO2]4 with PhIO in CH2Cl2. [Cp*2Mo2O5] was obtained by CH3COOH acidification of aqueous solutions of [Cp*MoO3]−Na+, the latter being generated in a single step from [Cp*MoCl4] and more than 5 equiv. of aqueous NaOH in air. Minor quantities of [Cp*MoO2]2 were also isolated from this reaction, although the formation of this by-product may be reduced by using a two-step basic hydrolysis procedure. Extension of the latter strategy also a…

MolybdenumAqueous solutionChemistrychemistry.chemical_elementBasic hydrolysisSingle stepRing (chemistry)Oxo ligandsMedicinal chemistryInorganic ChemistryCyclopentadienyl complexMolybdenumX-ray crystallography[CHIM.CRIS]Chemical Sciences/CristallographyOrganic chemistry[CHIM.COOR]Chemical Sciences/Coordination chemistryCyclopentadienyl ligandsX-ray crystallography
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A Bis(diazadiene) Adduct of MoCl 2 : Mononuclear, Octahedral, Undistorted and Diamagnetic

2004

The complex [MoCl2(iPr2dad)2] (iPr2dad = iPrN=CH−CH=N−iPr) is obtained in one step by reduction of [MoCl3(THF)3] in the presence of iPr2dad. The X-ray structure reveals a relatively undistorted octahedral coordination geometry with a relative cis configuration and points to a more appropriate description of the ligands as enediamides. The NMR investigation is in agreement with the same cis structure in solution and underlines the diamagnetism of the compound, at odds with previously reported very similar complexes. A bulk magnetic susceptibility measurement further confirms the compound’s diamagnetism. No equilibrium with a dinuclear, metal-metal bonded species is apparent from the solution…

MolybdenumDiazadiene ligands010405 organic chemistryChemistryLigandStereochemistry010402 general chemistry01 natural sciencesMagnetic susceptibilityX-ray diffraction0104 chemical sciencesAdductInorganic ChemistryCrystallographyOctahedronSpin stateDiamagnetismMolecule[CHIM.COOR]Chemical Sciences/Coordination chemistryCis–trans isomerismCoordination geometryEuropean Journal of Inorganic Chemistry
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Novel antiproliferative chimeric compounds with marked histone deacetylase inhibitory activity.

2014

Given our interest in finding potential antitumor agents and in view of the multifactorial mechanistic nature of cancer, in the present work, taking advantage of the multifunctional ligands approach, new chimeric molecules were designed and synthesized by combining in single chemical entities structural features of SAHA, targeting histone deacetylases (HDACs), with substituted stilbene or terphenyl derivatives previously obtained by us and endowed with antiproliferative and pro-apoptotic activity. The new chimeric derivatives were characterized with respect to their cytotoxic activity and their effects on cell cycle progression on different tumor cell lines, as well as their HDACs inhibitio…

Multifunctional ligandsCell cycle progressionHDAC inhibitionInhibitory postsynaptic potentialBiochemistrySettore BIO/13 - Biologia ApplicataHDACDrug DiscoverymedicineCytotoxic T cellHDAC inhibition; Multifunctional ligands; antiproliferative activity; chimeric compound; stilbeneCancerbiologyChemistryANTIPROLIFERATIVE ACTIVITYOrganic ChemistryMultifunctional ligandsCancermultifunctional ligandmedicine.diseaseCombinatorial chemistrySettore CHIM/08 - Chimica FarmaceuticastilbeneHistoneBiochemistrySTILBENESbiology.proteinchimeric compoundHDAC INHIBITORSEpigeneticsHistone deacetylaseChimeric molecules
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NHC-Based Iron Sensitizers for DSSCs

2018

International audience; Nanostructured dye-sensitized solar cells (DSSCs) are promising photovoltaic devices because of their low cost and transparency. Ruthenium polypyridine complexes have long been considered as lead sensitizers for DSSCs, allowing them to reach up to 11% conversion efficiency. However, ruthenium suffers from serious drawbacks potentially limiting its widespread applicability, mainly related to its potential toxicity and scarcity. This has motivated continuous research efforts to develop valuable alternatives from cheap earth-abundant metals, and among them, iron is particularly attractive. Making iron complexes applicable in DSSCs is highly challenging due to an ultrafa…

NHC ligands[CHIM.ORGA]Chemical Sciences/Organic chemistry[CHIM.COOR] Chemical Sciences/Coordination chemistry[CHIM.ORGA] Chemical Sciences/Organic chemistrylcsh:QD146-197[CHIM.THEO]Chemical Sciences/Theoretical and/or physical chemistry[CHIM.THEO] Chemical Sciences/Theoretical and/or physical chemistryiron complexes[CHIM] Chemical Scienceslcsh:Inorganic chemistry[CHIM]Chemical Sciences[CHIM.COOR]Chemical Sciences/Coordination chemistryexcited statesCèl·lules fotoelèctriquesphotophysicsFerro
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Surface Coordination of Multiple Ligands Endows N‐Heterocyclic Carbene‐Stabilized Gold Nanoclusters with High Robustness and Surface Reactivity

2020

Deciphering the molecular pictures of the multi-component and non-periodic organic-inorganic interlayer is a grand technical challenge. Here we show that the atomic arrangement of hybrid surface ligands on metal nanoparticles can be precisely quantified through comprehensive characterization of a novel gold cluster, Au 44 ( i Pr 2 -bimy) 9 (PA) 6 Br 8 , which features three types of ligands, namely, carbene (1,3-diisopropylbenzimidazolin-2-ylidene, i Pr 2 -bimy), alkynyl (phenylacetylide, PA), and halide (Br), respectively. The delicately balanced stereochemical effects and bonding capabilities of the three ligands give rise to peculiar geometrical and electronic structures. Remarkably, des…

Nanostructurecarbene ligandsHalidereaktiivisuus010402 general chemistry01 natural sciencesCatalysisCatalysisNanoclustersklusteritchemistry.chemical_compoundnanorakenteetnanostructuresCluster (physics)Gold clustercatalysis010405 organic chemistryChemistryGeneral MedicineGeneral Chemistry0104 chemical sciencesCrystallographykatalyysiYield (chemistry)rajapinnat (pinnat)cluster compoundssurface reactivitiesnanohiukkasetCarbeneAngewandte Chemie International Edition
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Half-sandwich molybdenum(III) compounds containing diazadiene ligands and their use in the controlled radical polymerization of styrene

2002

Abstract The reaction of CpMoCl2 with diazadiene ligands RNCHCHNR (R2dad) affords the corresponding paramagnetic complexes CpMoCl2(R2dad) (R=Ph, 1; p-Tol, 2; C6H3Pr2i-2,6, 3; and Pri, 4). All compounds have been characterized by EPR spectroscopy and have been investigated by cyclic voltammetry. They display one-electron oxidation and reduction processes, these being reversible or irreversible depending on the nature of R. The irreversibility of the reduction wave is due to a chemical follow-up process which consists of chloride loss from the reduced product. This phenomenon is suppressed in the presence of excess chloride in solution. An X-ray structure of 3 verifies the mononuclear na…

Nitroxide mediated radical polymerizationRadical polymerization010402 general chemistryPhotochemistry01 natural sciencesBiochemistryChlorideStyreneInorganic ChemistryLiving free-radical polymerizationchemistry.chemical_compoundCyclopentadienyl complexPolymer chemistryMaterials Chemistrymedicine[CHIM.COOR]Chemical Sciences/Coordination chemistryCyclopentadienylPhysical and Theoretical ChemistryControlled radical polymerizationMolybdenumDiazadiene ligands010405 organic chemistryChemistryOrganic Chemistry[CHIM.CATA]Chemical Sciences/Catalysis0104 chemical sciences[CHIM.POLY]Chemical Sciences/PolymersCobalt-mediated radical polymerizationPolymerizationParamagnetic organometallicsmedicine.drugJournal of Organometallic Chemistry
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Enantioselective Synthesis of 4-Substituted Dihydrocoumarins through a Zinc Bis(hydroxyamide)-Catalyzed Conjugate Addition of Terminal Alkynes

2013

A new enantioselective catalyst for the conjugate addition of terminal alkynes has been developed. Terminal alkynes react with 3-alkoxycarbonylcoumarins in the presence of diethylzinc and bis(hydroxyamide) ligands to give chiral non-racemic dihydrocoumarins substituted with an alkynyl group on the C-4 position with good yields and enantiomeric excesses up to 95%.

Nucleophilic additionChemistryStereochemistryN O ligandsEnantioselective synthesischemistry.chemical_elementAlkynylationGeneral ChemistryZincCatalysisOxygen heterocyclesAlkynylationFISICA APLICADAAsymmetric catalysismedia_common.cataloged_instanceEuropean unionNucleophilic additionmedia_commonConjugateAdvanced Synthesis & Catalysis
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Approaching ‘kit-type’ labelling with 68Ga : the DATA chelators.

2015

The DATA chelators are a novel class of tri-anionic ligands based on 6-amino-1,4-diazepine-triacetic acid, which have been introduced recently for the chelation of (68)Ga. Compared with macrocyclic chelators based on the cyclen scaffold (i.e., DOTA, DO3A, and DO2A derivatives), DATA chelators undergo quantitative radiolabelling more rapidly and under milder conditions. In this study, a systematic evaluation of the labelling of four DATA chelators--DATA(M), DATA(P), DATA(Ph), and DATA(PPh)--with (68)Ga is presented. The results highlight the extraordinary potential of this new class of chelators for application in molecular imaging using (68)Ga positron emission tomography (PET).

PharmacologyStereochemistryRadiopharmaceuticals.Organic ChemistryGallium-68Gallium RadioisotopesBiochemistryLigand designchemistry.chemical_compoundKineticsMacrocyclic ligandsCyclenchemistryLabellingIsotope LabelingDrug DiscoveryChelatesMolecular MedicineDOTAChelationGeneral Pharmacology Toxicology and PharmaceuticsMolecular imagingChelating Agents
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