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Haloperidol metabolite II prodrug: Asymmetric synthesis and biological evaluation on rat C6 glioma cells

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dc.contributor.author TURKEZ, Hasan
dc.date.accessioned 2015-01-07T12:18:52Z
dc.date.available 2015-01-07T12:18:52Z
dc.date.issued 2014-11-06
dc.identifier.uri http://openaccess.erzurum.edu.tr/xmlui/handle/123456789/30
dc.description.abstract In a previous work we 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)] via an ester bond. As a continua-tion of this work, here we report the asymmetric synthesis of compounds (R)-(þ)-MRJF4 and (S)-()-MRJF4 and the evaluation of their biological activity on rat C6 glioma cells, derived from glioblas toma multiforme (GBM), which is the most common and deadliest central nervous system (CNS) invasive malignancy. Favourable physicochemical properties, high permeability in the parallel artificial membrane permeability assay (PAMPA), good enzymatic and chemical stability, in vivo anticancer activity, associated with the capacity to reduce cell viability and to increase cell death by apoptosis, render compound (R)-(þ)-MRJF4 a promising candidate for the development of a useful therapeutic for gliomas therapy. tr_TR
dc.language.iso en tr_TR
dc.publisher http://www.sciencedirect.com/science/article/pii/S0223523414010344 tr_TR
dc.subject Glioma tr_TR
dc.subject HDAC tr_TR
dc.subject Sigma receptors tr_TR
dc.subject Inhibitors tr_TR
dc.subject Medicinal chemistry tr_TR
dc.title Haloperidol metabolite II prodrug: Asymmetric synthesis and biological evaluation on rat C6 glioma cells tr_TR
dc.title.alternative Haloperidol metaboliti II ön: sıçan C6 glioma hücreleri üzerinde Asimetrik sentez ve biyolojik değerlendirme tr_TR
dc.type Article tr_TR


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