6533b7dcfe1ef96bd1272083

RESEARCH PRODUCT

Synthesis and Antitumor Properties of 2,5-Bis(3'-indolyl) thiophenes: Analogues of Marine Alkaloid Nortopsentin

Ornella GiaAlessandra MontalbanoPatrizia DianaGaetano DattoloAnna CarboneLisa Dalla ViaPaola BarrajaGirolamo CirrincioneAnnamaria Martorana

subject

Cell typeIndolescyclizationHL60StereochemistryClinical BiochemistryPharmaceutical ScienceAntineoplastic AgentsThiophenesBiochemistryChemical synthesisInhibitory Concentration 50chemistry.chemical_compoundAlkaloids5-bis(3'-indolyl)thiophenesCell Line TumorDrug DiscoverymedicineAnimalsHumansantitumor activityMolecular BiologyCell Proliferationbis-indolylthiopheneCell growthNortopsentinMelanomaOrganic ChemistryImidazolesCancerBiological activityDNAmedicine.diseasediketonesTopoisomerase II5-bis(3'-indolyl)thiophenes; antitumor activity; Topoisomerase II; NortopsentinDNA Topoisomerases Type IIchemistryCell cultureMolecular Medicine

description

A series of 11 bis-indolylthiophenes of formula I were obtained by cyclization of bis-indole 1,4-diketones using Lawesson''s reagent. Derivs. I (R = OMe, R1 = SO2Ph), I (R = OMe, R1 = Me), I (R = Cl, R1 = Me), and I (R = OMe, R1 = H) were selected to be evaluated in the full panel of about 60 human tumor cell lines derived from nine human cancer cell types and showed antiproliferative activity generally in the micromolar range. The most sensitive cell lines were: CCRF-CEM, MOLT-4, HL60 (TB), and RPMI-8226 of the leukemia subpanel, HT29 and HCC-2998 cell lines of the colon sub-panel, NCI-H522 of the non-small cell lung cancer sub-panel, LOX IMVI of the melanoma sub-panel, and UO-31 of the renal cancer sub-panel.

yearjournalcountryeditionlanguage
2007-01-01
10.1016/j.bmcl.2007.01.065http://hdl.handle.net/10447/9215