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The anti-epileptic drug valproic acid harbors anti-tumoral activity in solid and leukemic tumor cell models and is currently evaluated in clinical trials. However, the plasma trough concentrations obtained in patients by common anti-epileptic dose regimens are below concentrations required for exerting anti-tumor effects in vitro. Here, we describe the identification of three novel valproic acid derivatives with superior differentiation-inducing and anti-proliferative activities in K562 bcr/abl-positive chronic myeloid leukemia cells and HL60 promyelocytic leukemia cells at achievable therapeutic VPA concentrations. These compounds reveal potent inhibition of histone deacetylase activity, induction of p21Cip/Waf expression as well as low toxicity on CD34+ bone marrow cells.

Titel:	Novel valproic acid derivatives with potent differentiation-inducing activity in myeloid leukemia cells.
Autor/in / Beteiligte Person:	Deubzer, H ; Busche, B ; Rönndahl, G ; Eikel, D ; Michaelis, M ; Cinatl, J ; Schulze, S ; Nau, H ; Witt, O
Link:	Zum Volltext
Zeitschrift:	Leukemia research, Jg. 30 (2006-09-01), Heft 9, S. 1167
Veröffentlichung:	Oxford ; New York : Pergamon Press, 2006
Medientyp:	academicJournal
ISSN:	0145-2126 (print)
DOI:	10.1016/j.leukres.2006.01.009
Schlagwort:	Anticonvulsants toxicity Antigens, CD34 Antineoplastic Agents toxicity Bone Marrow Cells enzymology Bone Marrow Cells pathology Cell Proliferation drug effects Cyclin-Dependent Kinase Inhibitor p21 biosynthesis Dose-Response Relationship, Drug Drug Screening Assays, Antitumor Fusion Proteins, bcr-abl biosynthesis Gene Expression Regulation, Enzymologic drug effects Gene Expression Regulation, Leukemic drug effects HL-60 Cells Histone Deacetylases biosynthesis Humans K562 Cells Leukemia, Myeloid enzymology Leukemia, Myeloid pathology Valproic Acid toxicity Anticonvulsants pharmacology Antineoplastic Agents pharmacology Cell Differentiation drug effects Leukemia, Myeloid drug therapy Valproic Acid analogs & derivatives Valproic Acid pharmacology
Sonstiges:	Nachgewiesen in: MEDLINE Sprachen: English Publication Type: Journal Article; Research Support, Non-U.S. Gov't Language: English [Leuk Res] 2006 Sep; Vol. 30 (9), pp. 1167-75. <i>Date of Electronic Publication: </i>2006 Feb 28. MeSH Terms: Anticonvulsants / pharmacology ; Antineoplastic Agents / pharmacology ; Cell Differentiation / drug effects ; Leukemia, Myeloid / drug therapy ; Valproic Acid / analogs & derivatives ; Valproic Acid / pharmacology ; Anticonvulsants / toxicity ; Antigens, CD34 ; Antineoplastic Agents / toxicity ; Bone Marrow Cells / enzymology ; Bone Marrow Cells / pathology ; Cell Proliferation / drug effects ; Cyclin-Dependent Kinase Inhibitor p21 / biosynthesis ; Dose-Response Relationship, Drug ; Drug Screening Assays, Antitumor ; Fusion Proteins, bcr-abl / biosynthesis ; Gene Expression Regulation, Enzymologic / drug effects ; Gene Expression Regulation, Leukemic / drug effects ; HL-60 Cells ; Histone Deacetylases / biosynthesis ; Humans ; K562 Cells ; Leukemia, Myeloid / enzymology ; Leukemia, Myeloid / pathology ; Valproic Acid / toxicity Substance Nomenclature: 0 (Anticonvulsants) ; 0 (Antigens, CD34) ; 0 (Antineoplastic Agents) ; 0 (CDKN1A protein, human) ; 0 (Cyclin-Dependent Kinase Inhibitor p21) ; 614OI1Z5WI (Valproic Acid) ; EC 2.7.10.2 (Fusion Proteins, bcr-abl) ; EC 3.5.1.98 (Histone Deacetylases) Entry Date(s): Date Created: 20060303 Date Completed: 20060912 Latest Revision: 20131121 Update Code: 20240513

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Novel valproic acid derivatives with potent differentiation-inducing activity in myeloid leukemia cells.