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  • Title: Novel valproic acid derivatives with potent differentiation-inducing activity in myeloid leukemia cells.
    Author: Deubzer H, Busche B, Rönndahl G, Eikel D, Michaelis M, Cinatl J, Schulze S, Nau H, Witt O.
    Journal: Leuk Res; 2006 Sep; 30(9):1167-75. PubMed ID: 16510182.
    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.
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