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.File in questo prodotto:
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