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Title: Design, synthesis, and biological evaluation of hybrid molecules containing α-methylene-γ-butyrolactones and α-bromoacryloyl moieties
Authors: Romagnoli, Romeo
Baraldi, Pier Giovanni
Tabrizi, Mojgan Aghazadeh
Bermejo, Jaime
Estévez, Francisco 
Borgatti, Monica
Gambari, Roberto
UNESCO Clasification: 32 Ciencias médicas
3209 Farmacología
2390 Química farmacéutica
Keywords: Benzoheterocyclic Derivatives
Antitumor Agents
Inhibitors, et al
Issue Date: 2005
Project: Nuevos Compuestos Antileucémicos 
Journal: Journal of Medicinal Chemistry 
Abstract: The synthesis and biological activity of hybrids 8-18 prepared combining alpha-methylene-gamma-butyrolactones and alpha-bromoacryloylamides have been described and their structure -activity relationships discussed. All these heterobifunctional compounds demonstrate good antileukemic activity, significantly superior to that of both alkylating units alone. Using the human leukemia HL-60 cell line, selected compounds 10, 11, 13, and 17 were found to induce morphological changes and internucleosomal DNA fragmentation characteristic of apoptotic cell death.
ISSN: 0022-2623
DOI: 10.1021/jm058012o
Source: Journal of Medicinal Chemistry [ISSN 0022-2623], v. 48 (24), p. 7906-7910 (Diciembre 2005)
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