6533b836fe1ef96bd12a096a

RESEARCH PRODUCT

SYNTHESIS AND ANTITUMOR ACTIVITY OF 2,5-BIS(3'-INDOLYL)-FURANS AND 3,5-BIS(3'-INDOLIY)-ISOXAZOLES, NORTOPSENTIN ANALOGUES

Heinz-herbert FiebigGerhard KelterGirolamo CirrincioneAnna CarbonePatrizia DianaPaola Barraja

subject

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

description

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.

yearjournalcountryeditionlanguage
2010-01-01
10.1016/j.bmc.2010.04.061https://hdl.handle.net/11567/1024298