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Novel Schiff base copper complexes of quinoline-2 carboxaldehyde as proteasome inhibitors in human prostate cancer cells

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JOURNAL OF MEDICINAL CHEMISTRY
卷 49, 期 24, 页码 7242-7246

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AMER CHEMICAL SOC
DOI: 10.1021/jm060712l

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We report the synthesis of novel 1: 1 Schiff base copper complexes of quinoline-2-carboxaldehyde showing dose-dependent, antiproliferative, and proapoptotic activity in PC-3 and LNCaP prostate cancer cells. We found that quinoline thiosemicarbazone 2 (FPA-137) was the most potent and inhibited proteosome activity in intact human prostate cancer PC-3 and LNCaP cells (IC50 of 4 and 3.2 mu M, respectively) compared to clioquinol and pyrrolidine dithiocarbamate (IC50 of 10 and 20 mu M), supporting the novelty of 2.

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