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• W2023404623 abstract "A series of N-hydroxy-3-phenyl-2-propenamides were prepared as novel inhibitors of human histone deacetylase (HDAC). These compounds were potent enzyme inhibitors, having IC50s < 400 nM in a partially purified enzyme assay. However, potency in cell growth inhibition assays ranged over 2 orders of magnitude in two human carcinoma cell lines. Selected compounds having cellular IC50 < 750 nM were tested for maximum tolerated dose (MTD) and for efficacy in the HCT116 human colon tumor xenograft assay. Four compounds having an MTD ≥ 100 mg/kg were selected for dose−response studies in the HCT116 xenograft model. One compound, 9 (NVP-LAQ824), had significant dose-related activity in the HCT116 colon and A549 lung tumor models, high MTD, and low gross toxicity. On the basis, in part, of these properties, 9 has entered human clinical trials in 2002." @default.
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• W2023404623 date "2003-09-13" @default.
• W2023404623 modified "2023-10-16" @default.
• W2023404623 title "<i>N</i>-Hydroxy-3-phenyl-2-propenamides as Novel Inhibitors of Human Histone Deacetylase with in Vivo Antitumor Activity: Discovery of (2<i>E</i>)-<i>N</i>-Hydroxy-3-[4-[[(2-hydroxyethyl)[2-(1<i>H</i>-indol-3-yl)ethyl]amino]methyl]phenyl]-2-propenamide (NVP-LAQ824)" @default.
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• W2023404623 doi "https://doi.org/10.1021/jm030235w" @default.
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