0000000000526270

AUTHOR

Finn K. Hansen

showing 2 related works from this author

In Vitro Assessment of the Genotoxic Hazard of Novel Hydroxamic Acid- and Benzamide-Type Histone Deacetylase Inhibitors (HDACi)

2020

Histone deacetylase inhibitors (HDACi) are already approved for the therapy of leukemias. Since they are also emerging candidate compounds for the treatment of non-malignant diseases, HDACi with a wide therapeutic window and low hazard potential are desirable. Here, we investigated a panel of 12 novel hydroxamic acid- and benzamide-type HDACi employing non-malignant V79 hamster cells as toxicology guideline-conform in vitro model. HDACi causing a &ge

DNA damageApoptosisHydroxamic AcidsDNA damage responseArticleCatalysisCell LineHistonesInorganic Chemistrylcsh:Chemistrychemistry.chemical_compoundHDAC inhibitorsCricetinaeDNA strand breaksmedicineAnimalsHumansDNA Breaks Double-StrandedDNA Breaks Single-StrandedPhosphorylationPhysical and Theoretical Chemistrynormal tissue toxicityMolecular BiologyVorinostatlcsh:QH301-705.5SpectroscopyVorinostatMicronucleus TestsHydroxamic acidMutagenicity TestsEntinostatOrganic ChemistryHistone H2AXgenetic instabilityGeneral MedicineComputer Science ApplicationsHistone Deacetylase Inhibitorschemistrylcsh:Biology (General)lcsh:QD1-999BenzamidesCancer researchComet AssayHistone deacetylasegenotoxic hazardDNAMutagensNucleotide excision repairmedicine.drugInternational Journal of Molecular Sciences
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Efficient synthesis and 5-LOX/COX-inhibitory activity of some 3-hydroxybenzo[b]thiophene-2-carboxylic acid derivatives

2012

Abstract A series of 3-hydroxybenzo[ b ]thiophene-2-carboxylic acid derivatives has been prepared and subsequently evaluated with regards to the inhibition of 5-LOX/COX. Structure optimization furnished derivatives with promising in vitro activity as dual 5-LOX/COX inhibitors with submicromolar IC 50 values for inhibition of 5-LOX and COX-1, respectively.

StereochemistryCarboxylic acidClinical BiochemistryCarboxylic AcidsPharmaceutical ScienceThiophenesInhibitory postsynaptic potentialBiochemistryStructure-Activity Relationshipchemistry.chemical_compoundDrug DiscoveryThiopheneCyclooxygenase InhibitorsLipoxygenase InhibitorsMolecular Biologychemistry.chemical_classificationArachidonate 5-Lipoxygenaseintegumentary systemOrganic Chemistryfood and beveragesBenzothiopheneIn vitrochemistryCyclooxygenase 1Molecular MedicineLicofeloneProtein BindingBioorganic & Medicinal Chemistry Letters
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