6533b856fe1ef96bd12b2f92

RESEARCH PRODUCT

ChemInform Abstract: Synthesis and Induction of G0-G1 Phase Arrest with Apoptosis of 3,5-Dimethyl-6-phenyl-8-(trifluoromethyl)-5,6-dihydropyrazolo[3,4-f] [1,2,3,5]tetrazepin-4(3H)-one.

Manlio TolomeoFabiana PlesciaSalvatrice MancusoDemetrio RaffaMaria Valeria RaimondiGiuliana CannizzoStella CascioferroEleonora BarbuscaGiuseppe DaidoneBenedetta Maggio

subject

Trifluoromethylmedicine.diagnostic_testHL60General MedicineMolecular biologyFlow cytometryMultiple drug resistancechemistry.chemical_compoundchemistryApoptosishemic and lymphatic diseasesmedicineBusulfanEtoposidemedicine.drugK562 cells

description

The multistep synthesis of 3,5-dimethyl-6-phenyl-8-(trifluoromethyl)-5,6-dihydropyrazolo[3,4-f][1,2,3,5]tetrazepin-4(3H)-one 15 has been carried out. The compound showed antiproliferative and apoptotic effects against K562, K562-R (imatinib mesilate resistant), HL60 and multidrug resistant (MDR) HL60 cell lines. Compound 15 showed a pro-apoptotic activity against HL60 and K562 resistant cell lines markedly higher than etoposide and busulfan, respectively. Flow cytometry studies carried out on K562 cells allowed to establish that 15 induces G0-G1 phase arrest followed by apoptosis.

yearjournalcountryeditionlanguage
2009-03-31ChemInform
https://doi.org/10.1002/chin.200913170