6533b7d7fe1ef96bd12690dc
RESEARCH PRODUCT
Synthesis and Antiproliferative Activity of 2,5-bis(3′-Indolyl)pyrroles, Analogues of the Marine Alkaloid Nortopsentin
Girolamo CirrincioneArmin MaierPaola BarrajaVirginia SpanòBarbara ParrinoPatrizia DianaAnna CarboneHeinz-herbert FiebigGerhard Keltersubject
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 alkaloidsdescription
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.
| year | journal | country | edition | language |
|---|---|---|---|---|
| 2013-03-01 | Marine Drugs |