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http://hdl.handle.net/10553/50569
| Título: | Design, synthesis, and biological evaluation of hybrid molecules containing α-methylene-γ-butyrolactones and α-bromoacryloyl moieties | Autores/as: | Romagnoli, Romeo Baraldi, Pier Giovanni Tabrizi, Mojgan Aghazadeh Bermejo, Jaime Estévez, Francisco Borgatti, Monica Gambari, Roberto |
Clasificación UNESCO: | 32 Ciencias médicas 3209 Farmacología 2390 Química farmacéutica |
Palabras clave: | Benzoheterocyclic Derivatives Antitumor Agents Distamycin Cells Inhibitors, et al. |
Fecha de publicación: | 2005 | Proyectos: | Nuevos Compuestos Antileucémicos | Publicación seriada: | Journal of Medicinal Chemistry | Resumen: | 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. | URI: | http://hdl.handle.net/10553/50569 | ISSN: | 0022-2623 | DOI: | 10.1021/jm058012o | Fuente: | Journal of Medicinal Chemistry [ISSN 0022-2623], v. 48 (24), p. 7906-7910 (Diciembre 2005) |
| Colección: | Artículos |
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