0000000000306906

AUTHOR

Gerhard Kelter

showing 3 related works from this author

Synthesis and Antiproliferative Activity of 2,5-bis(3′-Indolyl)pyrroles, Analogues of the Marine Alkaloid Nortopsentin

2013

2,5-bis(3′-Indolyl)pyrroles, analogues of the marine alkaloid nortopsentin, were conveniently prepared through a three step procedure in good overall yields. Derivatives 1a and 1b exhibited concentration-dependent antitumor activity towards a panel of 42 human tumor cell lines with mean IC50 values of 1.54 μM and 0.67 μM, respectively. Investigating human tumor xenografts in an ex-vivo clonogenic assay revealed selective antitumor activity, whereas sensitive tumor models were scattered among various tumor histotypes.

ex-vivo xenograftsIndolesStereochemistryPharmaceutical ScienceMice NudeAntineoplastic AgentsArticleInhibitory Concentration 50MiceCell Line TumorNeoplasmsDrug Discoverybis-indolyl-pyrroles; nortopsentin analogues; marine alkaloids; antitumor; <i>ex-vivo </i>xenograftsIc50 valuesAnimalsHumansnortopsentin analoguePyrrolesClonogenic assayPharmacology Toxicology and Pharmaceutics (miscellaneous)lcsh:QH301-705.5Tumor Stem Cell AssayMice nudeantitumorAntitumor activityDose-Response Relationship DrugChemistryAlkaloidbis-indolyl-pyrroles; nortopsentin analogues; marine alkaloids; antitumor; ex-vivo xenograftsImidazolesTumor Stem Cell AssaySettore CHIM/08 - Chimica FarmaceuticaXenograft Model Antitumor Assaysbis-indolyl-pyrrolemarine alkaloidHuman tumornortopsentin analogueslcsh:Biology (General)Cell culturebis-indolyl-pyrrolesmarine alkaloidsMarine Drugs
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SYNTHESIS AND ANTITUMOR ACTIVITY OF 2,5-BIS(3'-INDOLYL)-FURANS AND 3,5-BIS(3'-INDOLIY)-ISOXAZOLES, NORTOPSENTIN ANALOGUES

2010

Abstract A series of novel 2,5-bis(3′-indolyl)furans and 3,5-bis(3′-indolyl)isoxazoles were synthesized as antitumor agents. The antiproliferative activity was evaluated in vitro toward diverse human tumor cell lines. Initially 5 isoxazoles and 3 furan derivatives were tested against a panel of 10 human tumor cell lines and the most active derivatives 3c and 4a were selected to be evaluated in an extended panel of 29 cell lines. By exhibiting mean IC50 values of 17.4 μg/mL (3a) and 20.5 μg/mL (4c), in particular 4c showed a high level of tumor selectivity toward the 29 cell lines.

35-BIS(3'-INDOLIY)-ISOXAZOLESIndolesStereochemistry3Clinical Biochemistry2Pharmaceutical ScienceAntineoplastic AgentsBiochemistryChemical synthesis25-BIS(3'-INDOLYL)-FURANSchemistry.chemical_compound2; 5-BIS(3'-INDOLYL)-FURANS; 3; 5-BIS(3'-INDOLIY)-ISOXAZOLES; NORTOPSENTIN; ANTITUMOR ACTIVITYFuranCell Line TumorNeoplasmsDrug DiscoveryHumans5-BIS(3'-INDOLIY)-ISOXAZOLESCytotoxicityFurans5-BIS(3'-INDOLYL)-FURANSMolecular BiologyAntitumor activityAlkaloidOrganic ChemistryBiological activityNORTOPSENTINIsoxazolesSettore CHIM/08 - Chimica FarmaceuticaIn vitroANTITUMOR ACTIVITYchemistryCell cultureMolecular MedicineDrug Screening Assays Antitumor
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Pharmacogenomics of cantharidin in tumor cells.

2014

Cantharis vesicatoria (blister beetle) is used in Chinese medicine and has been categorized as highly toxic in the Chinese pharmacopeia. In Europe, Cantharis patches have been used since ages to treat various skin-related diseases. We investigated the cytotoxicity of the Cantharis ingredient, cantharidin, in 41 tumor cell lines (Oncotest panel) and compared the results with those of 60 cell lines of the National Cancer Institute, USA. We found profound activity at low micromolar concentrations (log ₁₀IC₅₀ values between -6.980 and 5.009 M). Cantharidin bound to protein phosphatase 2A (PP2A) with higher affinity (-8.12 kcal/mol) than to PP1 (-6.25 kcal/mol) in molecular docking analyses. Usi…

Models MolecularProtein ConformationBlister beetleBiologyCantharisBiochemistryFas ligandGene Expression Regulation Enzymologicchemistry.chemical_compoundCell Line TumorGene expressionAnimalsHumansRNA MessengerCytotoxicityOligonucleotide Array Sequence AnalysisPharmacologyCantharidinBinding SitesMolecular Structurebiology.organism_classificationMolecular biologyReceptors Neuropeptide YchemistryCell cultureApoptosisPharmacogeneticsImmunologyCantharidinBiochemical pharmacology
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