6533b7d0fe1ef96bd125a8ac

RESEARCH PRODUCT

Synthesis and antiproliferative activities of two new analogs of tetrazepinones

Maria Valeria RaimondiBenedetta MaggioDemetrio RaffaFabiana PlesciaStefania GrimaudoM TolomeoGiuseppe Daidone

subject

Telozolomide 35-dimethyl-6-phenyl-8-(trifluoromethyl-56-dihydropyrazo1o[3-4-f]1235)tetrazepin-4(3H)-one 3-(2-chloroethyl)-5-methyl-6-phenyl-8-(trifluoromethyl-56-dihydropyrazo1o[3-4-f]1235)tetrazepin-4(3H)-one pro-apoptotic activity G0-G1 phase arrestSettore BIO/10 - BiochimicaSettore CHIM/08 - Chimica Farmaceutica

description

Based on the encouraging results, we report the multistep synthesis and the biologicalo results of two new analogs of tetrazepinones: the 3,5-dimethyl-6-phenyl-8-(trifluoromethyl-5,6-dihydropyrazo1o[3-4-f]1,2,35)tetrazepin-4(3H)-one and the 3-(2-chloroethyl)-5-methyl-6-phenyl-8-(trifluoromethyl-5,6-dihydropyrazo1o[3-4-f]1,2,35)tetrazepin-4(3H)-one. Both compounds showed a pro-apoptotic activity against HL60 and K562 resistant cell lines. Flow cytometry studies carried out 0n K562 cells allowed to establish that the methyl derivative induces G0-G1, phase arrest followed by apoptosis, whereas the chloroethyl derivative is a not phase-specific agent.

yearjournalcountryeditionlanguage
http://hdl.handle.net/10447/230435