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

Risultato della ricerca: Article

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 originaleEnglish
pagine (da-a)2386-2394
Numero di pagine9
RivistaEuropean Journal of Medicinal Chemistry
Volume43
Stato di pubblicazionePublished - 2008

Fingerprint

Cell Cycle Resting Phase
K562 Cells
G1 Phase
Cells
Apoptosis
Cell Line
Busulfan
Mesylates
Flow cytometry
HL-60 Cells
Etoposide
Flow Cytometry
3,5-dimethyl-6-phenyl-8-(trifluoromethyl)-5,6-dihydropyrazolo(3,4-f)(1,2,3,5)tetrazepin-4(3H)-one
Imatinib Mesylate

All Science Journal Classification (ASJC) codes

  • Pharmacology
  • Organic Chemistry
  • Drug Discovery

Cita questo

@article{a3c3c8ef37db45c9876901705d742b25,
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.",
keywords = "1,2,3,4-Tetrazepinones; Pyrazolo[3,4-f][1,2,3,4]tetrazepinones; Drug resistance; G0-G1 arrest; Apoptosis; Antiproliferative activity",
author = "Giuseppe Daidone and Demetrio Raffa and Fabiana Plescia and Cascioferro, {Stella Maria} and Salvatrice Mancuso and Raimondi, {Maria Valeria}",
year = "2008",
language = "English",
volume = "43",
pages = "2386--2394",
journal = "European Journal of Medicinal Chemistry",
issn = "0223-5234",
publisher = "Elsevier Masson SAS",

}

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 - Daidone, Giuseppe

AU - Raffa, Demetrio

AU - Plescia, Fabiana

AU - Cascioferro, Stella Maria

AU - Mancuso, Salvatrice

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 - 1,2,3,4-Tetrazepinones; Pyrazolo[3,4-f][1,2,3,4]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 -