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

Deubzer, Hedwig, Busche, Barbara, Rönndahl, Gabi, Eikel, Daniel, Michaelis, Martin, Cinatl, Jindrich, Schulze, Sandra, Nau, Heinz, Witt, Olaf (2006) Novel valproic acid derivatives with potent differentiation-inducing activity in myeloid leukemia cells. Leukemia research, 30 (9). pp. 1167-75. ISSN 0145-2126. (The full text of this publication is not currently available from this repository. You may be able to access a copy if URLs are provided)

The full text of this publication is not currently available from this repository. You may be able to access a copy if URLs are provided. (Contact us about this Publication)

Abstract

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.

Item Type: Article
Subjects: R Medicine > RM Therapeutics. Pharmacology
Divisions: Faculties > Sciences > School of Biosciences
Depositing User: Martin Michaelis
Date Deposited: 05 Jun 2013 20:54 UTC
Last Modified: 29 May 2019 10:14 UTC
Resource URI: https://kar.kent.ac.uk/id/eprint/34099 (The current URI for this page, for reference purposes)
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