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000867366 1001_ $$0P:(DE-HGF)0$$aKrieger, Viktoria$$b0
000867366 245__ $$aSynthesis of peptoid-based class I selective histone deacetylase inhibitors with chemosensitizing properties
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000867366 520__ $$aThere is increasing evidence that histone deacetylase (HDAC) inhibitors can (re)sensitize cancer cells for chemotherapeutics via ‘epigenetic priming’. In this work, we describe the synthesis of a series of class I selective HDAC inhibitors with 2-aminoanilides as zinc-binding groups. Several of the synthesized compounds revealed potent inhibition of the class I HDAC isoforms HDAC1, 2 and/or 3 and promising antiproliferative effects in the human ovarian cancer cell line A2780 and the human squamous carcinoma cell line Cal27. Selected compounds were investigated in a cellular model of platinum resistance. In particular compound 2a revealed potent chemosensitizing properties and full reversal of cisplatin resistance in Cal27CisR cells. This effect is related to a synergistic increase in caspase 3/7 activation and induction of apoptosis. Thus, this work demonstrates that pan-HDAC inhibition or dual class I/class IIb inhibition is not required for full reversal of cisplatin resistance.
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000867366 7001_ $$0P:(DE-HGF)0$$aHamacher, Alexandra$$b1
000867366 7001_ $$0P:(DE-HGF)0$$aCao, Fangyuan$$b2
000867366 7001_ $$0P:(DE-HGF)0$$aStenzel, Katharina$$b3
000867366 7001_ $$0P:(DE-Juel1)174133$$aGertzen, Christoph G. W.$$b4$$ufzj
000867366 7001_ $$0P:(DE-HGF)0$$aSchäker-Hübner, Linda$$b5
000867366 7001_ $$0P:(DE-HGF)0$$aKurz, Thomas$$b6
000867366 7001_ $$0P:(DE-Juel1)172663$$aGohlke, Holger$$b7$$ufzj
000867366 7001_ $$0P:(DE-HGF)0$$aDekker, Frank J.$$b8
000867366 7001_ $$0P:(DE-HGF)0$$aKassack, Matthias U.$$b9$$eCorresponding author
000867366 7001_ $$0P:(DE-HGF)0$$aHansen, Finn K.$$b10$$eCorresponding author
000867366 773__ $$0PERI:(DE-600)1491411-6$$a10.1021/acs.jmedchem.9b01489$$gp. acs.jmedchem.9b01489$$n24$$p11260-11279$$tJournal of medicinal chemistry$$v62$$x1520-4804$$y2019
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