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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.


Maria Dichiara, Emanuele Amata, Antonio Rescifina, Orazio Prezzavento, Giuseppe Floresta, Carmela Parenti, Valeria Pittalà, Agostino Marrazzo. Synthesis and evaluation of haloperidol metabolite II prodrugs as anticancer agents. Future medicinal chemistry. 2017 Oct;9(15):1749-1764

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PMID: 28869398

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