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

Salvatrice Mancuso; Fabiana Plescia; Giuseppe Daidone; Stella Maria Cascioferro; Benedetta Maggio; Demetrio Raffa; Maria Valeria Raimondi

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

Salvatrice Mancuso, Fabiana Plescia, Giuseppe Daidone, Stella Maria Cascioferro, Benedetta Maggio, Demetrio Raffa, Maria Valeria Raimondi

Promozione della Salute, Materno-Infantile, di Medicina Interna e Specialistica di Eccellenza “G. D’Alessandro”
Scienze e Tecnologie Biologiche Chimiche e Farmaceutiche

Risultato della ricerca: Article › peer review

14 Citazioni (Scopus)

Abstract

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.

Lingua originale	English
pagine (da-a)	2386-2394
Numero di pagine	9
Rivista	European Journal of Medicinal Chemistry
Volume	43
Stato di pubblicazione	Published - 2008

All Science Journal Classification (ASJC) codes

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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. / Mancuso, Salvatrice ; Plescia, Fabiana ; Daidone, Giuseppe ; Cascioferro, Stella Maria ; Maggio, Benedetta ; Raffa, Demetrio ; Raimondi, Maria Valeria.

In: European Journal of Medicinal Chemistry, Vol. 43, 2008, pag. 2386-2394.

Risultato della ricerca: Article › peer review

Mancuso, Salvatrice ; Plescia, Fabiana ; Daidone, Giuseppe ; Cascioferro, Stella Maria ; Maggio, Benedetta ; Raffa, Demetrio ; Raimondi, Maria Valeria. / 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. In: European Journal of Medicinal Chemistry. 2008 ; Vol. 43. pagg. 2386-2394.

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title = "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",

abstract = "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.",

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author = "Salvatrice Mancuso and Fabiana Plescia and Giuseppe Daidone and Cascioferro, {Stella Maria} and Benedetta Maggio and Demetrio Raffa and Raimondi, {Maria Valeria}",

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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

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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.

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KW - 2

KW - 3

KW - 4-Tetrazepinones; Pyrazolo[3

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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

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JO - European Journal of Medicinal Chemistry

JF - European Journal of Medicinal Chemistry

SN - 0223-5234

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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

Abstract

All Science Journal Classification (ASJC) codes

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