6533b7d4fe1ef96bd1262984

RESEARCH PRODUCT

Synthesis and Antiproliferative Activity of Novel 3-(Indazol-3-yl)-quinazolin-4(3H)-one and 3-(Indazol-3-yl)-benzotriazin-4(3H)-one Derivatives

Benedetta MaggioGiuseppe DaidoneFabiana PlesciaDemetrio RaffaDomenico Schillaci

subject

IndazolesMagnetic Resonance SpectroscopyChemical PhenomenaBicyclic moleculeChemistry PhysicalTriazinesCell growthStereochemistryPharmaceutical ScienceAntineoplastic AgentsChemical synthesisIn vitrochemistry.chemical_compoundchemistryCell cultureDrug DiscoveryQuinazolinesTumor Cells CulturedLactamHumansGrowth inhibitionIC50

description

Several new 3-(indazol-3-yl)-quinazolin-4(3H)-one and 3-(indazol-3-yl)-benzotriazin-4(3H)-one derivatives 5 and 6 were synthesized and tested for their in vitro antiproliferative activity against Raji, K562, and K562-R cell lines. The pharmacological screening showed that some 2, 6, or 7-substituted quinazolinones 5 posses a significant antiproliferative activity, with a percentage growth inhibition ranging from 44.8% to 100% at 50 microM, which was higher than that showed by the unsubstituted derivative 5a previously synthesized. For the most active compounds 5d, 5f, and 5g the IC50 were recorded.

yearjournalcountryeditionlanguage
1999-10-16Archiv der Pharmazie
https://doi.org/10.1002/(sici)1521-4184(19999)332:9<317::aid-ardp317>3.0.co;2-r