0000000000777929

AUTHOR

Claudia Martini

0000-0001-9379-3027

showing 3 related works from this author

Two mixed valence diruthenium(ii,iii) isomeric complexes show different anticancer properties

2021

In this paper it is demonstrated that the nature of the ligands of two Ru2(II,III) paddlewheel complexes dramatically affects the overall anticancer properties in cells. Herein, the complex [Ru2(EB776)4Cl] was found to be more active against a glioblastoma model with respect to its isomer [Ru2(EB106)4Cl]. These different effects depend on the steric hindrance, on the allowed conformations of the complexes and on the presence of hydrophilic regions in [Ru2(EB776)4Cl], which overall lead to a lower “steric protection”.

Inorganic ChemistrySteric effectsValence (chemistry)StereochemistryChemistrymedicinemedicine.diseaseGlioblastoma
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Synthesis, benzodiazepine receptor binding and molecular modelling of isochromeno[4,3-c]pyrazol-5(1H)-one derivatives

2012

Abstract A series of isochromeno[4,3-c]pyrazole-5(1H)-one derivatives 7b–h were prepared and tested at 10 μM for their ability to displace specific [3H]flunitrazepam from bovine brain membranes. The substitution pattern of the above derivatives was shown to influence the receptor affinity. The most active compound of the series was 7e, showing a 54% inhibition of [3H]flunitrazepam binding. Compounds 7a–d,i were compared with the known isomers chromeno[4,3-c]pyrazole-4(1H)-ones 14a–d,i, showing that the isochromene/chromene isomerism influences the activity.

StereochemistryProtein ConformationChemistry Techniques SyntheticIsochromeno[43-c]pirazoles Dihydrospiro[isoindole-13’-pyrazol]-3(2H)- ones Benzodiazepine receptorDrug DiscoverymedicineAnimalsHumansBenzopyransReceptorBenzodiazepine receptor bindingPharmacologyChemistryOrganic ChemistryGeneral MedicineReceptors GABA-ASettore CHIM/08 - Chimica FarmaceuticaMolecular Docking SimulationMembraneBovine brainActive compoundPyrazolesCattleFlunitrazepam bindingFlunitrazepammedicine.drugProtein Binding
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ChemInform Abstract: Synthesis, Benzodiazepine Receptor Binding and Molecular Modelling of Isochromeno[4,3-c]pyrazol-5(1H)-one Derivatives.

2012

A series of isochromeno[4,3-c]pyrazol-5(1H)-one derivatives (III) is prepared and tested for their ability to displace specific [3H]flunitrazepam from bovine brain membranes.

MembraneBovine brainChemistryStereochemistrymedicineGeneral MedicineFlunitrazepamBenzodiazepine receptor bindingmedicine.drugChemInform
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