Synthesis of 10 pyrroloiminoquinone derivatives is presented. The strategy is based around the elaboration of a common intermediate by reaction with primary amines. All the compounds obtained have been subjected to antiproliferative activity with three different cell lines (NCI-H460, HeLa, and HL-60). The capacity of 4 selected compounds to affect the enzymatic activity of the nuclear enzyme DNA topoisomerase II and to form the typical DNA fragmentation which occurs in the apoptotic process is discussed here.

Synthesis and biological evaluation of pyrroloiminoquinone derivatives / D. Passarella, F. Belinghieri, M. Scarpellini, G. Pratesi, F. Zunino, O.M. Gia, L. Dalla Via, G. Santoro, B. Danieli. - In: BIOORGANIC & MEDICINAL CHEMISTRY. - ISSN 0968-0896. - 2008:5(2008 Mar), pp. 2431-2438.

Synthesis and biological evaluation of pyrroloiminoquinone derivatives

D. Passarella
Primo
;
F. Belinghieri
Secondo
;
M. Scarpellini;B. Danieli
Ultimo
2008

Abstract

Synthesis of 10 pyrroloiminoquinone derivatives is presented. The strategy is based around the elaboration of a common intermediate by reaction with primary amines. All the compounds obtained have been subjected to antiproliferative activity with three different cell lines (NCI-H460, HeLa, and HL-60). The capacity of 4 selected compounds to affect the enzymatic activity of the nuclear enzyme DNA topoisomerase II and to form the typical DNA fragmentation which occurs in the apoptotic process is discussed here.
Antiproliferative activity; DNA fragmentation; Pyrroloiminoquinone derivatives; Topoisomerase II
Settore CHIM/06 - Chimica Organica
mar-2008
Article (author)
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Utilizza questo identificativo per citare o creare un link a questo documento: https://hdl.handle.net/2434/35401
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