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001     867366
005     20210130003724.0
024 7 _ |a 10.1021/acs.jmedchem.9b01489
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100 1 _ |a Krieger, Viktoria
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245 _ _ |a Synthesis of peptoid-based class I selective histone deacetylase inhibitors with chemosensitizing properties
260 _ _ |a Washington, DC
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520 _ _ |a There is increasing evidence that histone deacetylase (HDAC) inhibitors can (re)sensitize cancer cells for chemotherapeutics via ‘epigenetic priming’. In this work, we describe the synthesis of a series of class I selective HDAC inhibitors with 2-aminoanilides as zinc-binding groups. Several of the synthesized compounds revealed potent inhibition of the class I HDAC isoforms HDAC1, 2 and/or 3 and promising antiproliferative effects in the human ovarian cancer cell line A2780 and the human squamous carcinoma cell line Cal27. Selected compounds were investigated in a cellular model of platinum resistance. In particular compound 2a revealed potent chemosensitizing properties and full reversal of cisplatin resistance in Cal27CisR cells. This effect is related to a synergistic increase in caspase 3/7 activation and induction of apoptosis. Thus, this work demonstrates that pan-HDAC inhibition or dual class I/class IIb inhibition is not required for full reversal of cisplatin resistance.
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700 1 _ |a Hamacher, Alexandra
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700 1 _ |a Cao, Fangyuan
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700 1 _ |a Stenzel, Katharina
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700 1 _ |a Gertzen, Christoph G. W.
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700 1 _ |a Schäker-Hübner, Linda
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700 1 _ |a Kurz, Thomas
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700 1 _ |a Gohlke, Holger
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700 1 _ |a Dekker, Frank J.
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700 1 _ |a Kassack, Matthias U.
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700 1 _ |a Hansen, Finn K.
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773 _ _ |a 10.1021/acs.jmedchem.9b01489
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|t Journal of medicinal chemistry
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