The synthesis and biol. activity of hybrids I (X = NH, NMe, O, S; R = Me, Ph, 4-ClC6H4, 4-PhC6H4) combining -methylene--butyrolactone and -bromoacryloylamide units have been synthesized and their structure-activity relationship has been studied. All these heterobifunctional compds. demonstrate good antileukemic activity, significantly superior to that of both alkylating units alone. Using the human leukemia HL-60 cell line, selected compds. were found to induce morphol. changes and internucleosomal DNA fragmentation characteristic of apoptotic cell death.

Design, synthesis, and biological evaluation of hybrid molecules containing alpha-methylene-gamma-butyrolactones and alpha-bromoacryloyl moieties

ROMAGNOLI, Romeo;BARALDI, Pier Giovanni;AGHAZADEH TABRIZI, Mojgan;BORGATTI, Monica;GAMBARI, Roberto
2005

Abstract

The synthesis and biol. activity of hybrids I (X = NH, NMe, O, S; R = Me, Ph, 4-ClC6H4, 4-PhC6H4) combining -methylene--butyrolactone and -bromoacryloylamide units have been synthesized and their structure-activity relationship has been studied. All these heterobifunctional compds. demonstrate good antileukemic activity, significantly superior to that of both alkylating units alone. Using the human leukemia HL-60 cell line, selected compds. were found to induce morphol. changes and internucleosomal DNA fragmentation characteristic of apoptotic cell death.
2005
Romagnoli, Romeo; Baraldi, Pier Giovanni; AGHAZADEH TABRIZI, Mojgan; Bermejo, J; Estevez, F; Borgatti, Monica; Gambari, Roberto
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Utilizza questo identificativo per citare o creare un link a questo documento: https://hdl.handle.net/11392/516657
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