On January 27, 2015, Sozio, Piera; Fiorito, Jole; Di Giacomo, Viviana; Di Stefano, Antonio; Marinelli, Lisa; Cacciatore, Ivana; Cataldi, Amelia; Pacella, Stephanie; Turkez, Hasan; Parenti, Carmela; Rescifina, Antonio; Marrazzo, Agostino published an article.Computed Properties of 39512-49-7 The title of the article was Haloperidol metabolite II prodrug: Asymmetric synthesis and biological evaluation on rat C6 glioma cells. And the article contained the following:
In a previous work the authors reported the antiproliferative effects of (±)-MRJF4, a novel haloperidol metabolite II (HP-mII) (a sigma-1 antagonist and sigma-2 agonist) prodrug, obtained through conjugation to 4-phenylbutyric acid (PhBA) [a histone deacetylase inhibitor (HDACi)] by an ester bond. As a continuation of this work, here the authors report the asym. synthesis of compounds Benzenebutanoic acid 4-[(1R)-4-(4-chlorophenyl)-4-hydroxy-1-piperidinyl]-1-(4-fluorophenyl)butyl ester [(R)-(+)-MRJF4] and 4-[(1R)-4-(4-chlorophenyl)-4-hydroxy-1-piperidinyl]-1-(4-fluorophenyl)butyl ester [(S)-(-)-MRJF4] and the evaluation of their biol. activity on rat C6 glioma cells, derived from glioblastoma multiforme (GBM), which is the most common and deadliest central nervous system (CNS) invasive malignancy. Favorable physicochem. properties, high permeability in the parallel artificial membrane permeability assay (PAMPA), good enzymic and chem. stability, in vivo anticancer activity, associated with the capacity to reduce cell viability and to increase cell death by apoptosis, render compound (R)-(+)-MRJF4 a promising candidate for the development of a useful therapeutic for glioma therapy. The synthesis of the target compounds was achieved by a reaction of (αS)-4-(4-chlorophenyl)-α-(4-fluorophenyl)-4-hydroxy-1-piperidienbutanol or (αR)-4-(4-chlorophenyl)-α-(4-fluorophenyl)-4-hydroxy-1-piperidienbutanol with benzenebutanoyl chloride. The experimental process involved the reaction of 4-(4-Chlorophenyl)piperidin-4-ol(cas: 39512-49-7).Computed Properties of 39512-49-7
The Article related to haloperidol metabolite prodrug anticancer antitumor glioma, benzenebutanoic acid hydroxypiperidine preparation anticancer agent cns glioma, glioma, hdac, inhibitors, medicinal chemistry, sigma receptors and other aspects.Computed Properties of 39512-49-7
Referemce:
Piperidine – Wikipedia,
Piperidine | C5H11N – PubChem