TY - JOUR
T1 - 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
AU - Mancuso, Salvatrice
AU - Plescia, Fabiana
AU - Daidone, Giuseppe
AU - Cascioferro, Stella Maria
AU - Maggio, Benedetta
AU - Raffa, Demetrio
AU - Raimondi, Maria Valeria
PY - 2008
Y1 - 2008
N2 - 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.
AB - 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.
KW - 1
KW - 2
KW - 3
KW - 4-Tetrazepinones; Pyrazolo[3
KW - 4-f][1
KW - 4]tetrazepinones; Drug resistance; G0-G1 arrest; Apoptosis; Antiproliferative activity
KW - 1
KW - 2
KW - 3
KW - 4-Tetrazepinones; Pyrazolo[3
KW - 4-f][1
KW - 4]tetrazepinones; Drug resistance; G0-G1 arrest; Apoptosis; Antiproliferative activity
UR - http://hdl.handle.net/10447/39024
M3 - Article
VL - 43
SP - 2386
EP - 2394
JO - European Journal of Medicinal Chemistry
JF - European Journal of Medicinal Chemistry
SN - 0223-5234
ER -