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    Keywords: CANCER ; CELLS ; EXPRESSION ; IN-VITRO ; proliferation ; tumor ; CLINICAL-TRIAL ; Germany ; INHIBITION ; MODEL ; MODELS ; TOXICITY ; VITRO ; DRUG ; DIFFERENTIATION ; PATIENT ; INDUCTION ; bone marrow ; BONE-MARROW ; ACID ; TRIAL ; TRIALS ; IDENTIFICATION ; PLASMA ; CLINICAL-TRIALS ; leukemia ; DERIVATIVES ; HUMAN NEUROBLASTOMA-CELLS ; HDAC ; LEUKEMIA-CELLS ; RE ; DEACETYLASE ; TUMOR-CELL ; HISTONE DEACETYLASE INHIBITORS ; TRANSFORMED-CELLS ; ANALOGS ; bone marrow cells ; K562 ; BONE ; ANTITUMOR ; valproic acid ; FETAL-HEMOGLOBIN EXPRESSION ; HL60 ; p21(Cip/Waf) ; SODIUM VALPROATE ; VPA
    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 P21(Cip/Waf) expression as well as low toxicity on CD34(+) bone marrow cells. (c) 2006 Elsevier Ltd. All rights reserved
    Type of Publication: Journal article published
    PubMed ID: 16510182
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