Dichiara Maria, Amata Emanuele, Rescifina Antonio, Prezzavento Orazio, Floresta Giuseppe, Parenti Carmela, Pittalà Valeria, Marrazzo Agostino
Dipartimento di Scienze del Farmaco, Università di Catania, Viale Andrea Doria 6, 95125 Catania, Italy.
Dipartimento di Scienze Chimiche, Università di Catania, Viale Andrea Doria 6, 95125 Catania, Italy.
Future Med Chem. 2017 Oct;9(15):1749-1764. doi: 10.4155/fmc-2017-0064. Epub 2017 Sep 4.
The use of haloperidol metabolite II (HP-metabolite II) prodrugs is an emerging strategy in the treatment of cancer. HP-metabolite II exhibits antiproliferative properties at micromolar concentrations inducing apoptosis in different types of cancer. Thus, the application of the prodrug approach appears as a useful method leading to much more desirable pharmacokinetic and pharmacodynamic properties. Some studies have shown that the esterification of the hydroxyl group of HP-metabolite II with 4-phenylbutiric acid (4-PBA) or valproic acid enhances the anticancer therapeutic potency. The current progresses in the design, synthesis and evaluation of anticancer activity of HP metabolite II prodrugs will be discussed in this review.
使用氟哌啶醇代谢物II（HP-代谢物II）前药是癌症治疗中的一种新兴策略。HP-代谢物II在微摩尔浓度下表现出抗增殖特性，可诱导不同类型癌症的细胞凋亡。因此，前药方法的应用似乎是一种有用的方法，可带来更理想的药代动力学和药效学特性。一些研究表明，HP-代谢物II的羟基与4-苯基丁酸（4-PBA）或丙戊酸酯化可增强抗癌治疗效力。本文将讨论HP代谢物II前药在设计、合成和抗癌活性评估方面的当前进展。
