Piperazine derivatives of butyric acid as differentiating agents in human leukemic cells

Cancer Chemotherapy and Pharmacology
R GilletF Pieri

Abstract

Butyric acid is a potent antineoplastic agent with a well-documented differentiation activity on a wide variety of tumor cells. However, its clinical development is strongly limited by its very short metabolic half-life. In this study we report on the in vitro effects of new original piperazine derivatives of butyric acid on the induction of differentiation and the growth inhibition of human erythroleukemia K562 cells and myeloid leukemia HL60 cells. 1-(2-hydroxyethyl) 4-(1-oxobutyl)-piperazine (HEPB) and [1-(2-hydroxyethyl) 4-(1-oxobutyl)-piperazine] butyrate (HEPDB) were efficient in acting on the differentiation and proliferation of both cell lines, whereas 1-phenyl 4-(1-oxobutyl)-piperazine (PPB) and 1-(3,4-methylene dioxybenzyl) 4-(1-oxobutyl)-piperazine (POB) acted only on proliferation rates. Such derivatives did not induce significant toxicity in mice. These preliminary results should enable, by the development of new series of piperazine derivatives, a better understanding of the mechanisms of action of butyric acid and its analogues on the coupling of growth and differentiation of neoplastic cells.

Citations

Dec 3, 2013·Spectrochimica Acta. Part A, Molecular and Biomolecular Spectroscopy·N PrabavathiV Krishnakumar
Aug 25, 2001·Cancer Letters·O WittA Pekrun
Sep 4, 2012·International Journal of Molecular Sciences·Mine YarimRengul Atalay
Feb 24, 2015·Journal of Enzyme Inhibition and Medicinal Chemistry·Halise Inci GulHiroshi Sakagami
Jul 9, 2008·Journal of Enzyme Inhibition and Medicinal Chemistry·C S Ananda KumarK S Rangappa
Sep 23, 2003·Expert Opinion on Therapeutic Targets·Karl J TronstadØystein Bruserud

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