Romagnoli Romeo, Baraldi Pier Giovanni, Tabrizi Mojgan Aghazadeh, Bermejo Jaime, Estévez Francisco, Borgatti Monica, Gambari Roberto
Dipartimento di Scienze Farmaceutiche, Università di Ferrara, 44100 Ferrara, Italy.
J Med Chem. 2005 Dec 1;48(24):7906-10. doi: 10.1021/jm058012o.
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.
已描述了结合α-亚甲基-γ-丁内酯和α-溴丙烯酰胺制备的杂化物8-18的合成及生物活性，并讨论了它们的构效关系。所有这些异双功能化合物均表现出良好的抗白血病活性，明显优于单独的两种烷基化单元。使用人白血病HL-60细胞系，发现所选化合物10、11、13和17可诱导凋亡细胞死亡特征性的形态变化和核小体间DNA片段化。
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