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@ARTICLE{Krieger:867366,
      author       = {Krieger, Viktoria and Hamacher, Alexandra and Cao, Fangyuan
                      and Stenzel, Katharina and Gertzen, Christoph G. W. and
                      Schäker-Hübner, Linda and Kurz, Thomas and Gohlke, Holger
                      and Dekker, Frank J. and Kassack, Matthias U. and Hansen,
                      Finn K.},
      title        = {{S}ynthesis of peptoid-based class {I} selective histone
                      deacetylase inhibitors with chemosensitizing properties},
      journal      = {Journal of medicinal chemistry},
      volume       = {62},
      number       = {24},
      issn         = {1520-4804},
      address      = {Washington, DC},
      publisher    = {ACS},
      reportid     = {FZJ-2019-06042},
      pages        = {11260-11279},
      year         = {2019},
      abstract     = {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.},
      cin          = {NIC / JSC / ICS-6},
      ddc          = {610},
      cid          = {I:(DE-Juel1)NIC-20090406 / I:(DE-Juel1)JSC-20090406 /
                      I:(DE-Juel1)ICS-6-20110106},
      pnm          = {511 - Computational Science and Mathematical Methods
                      (POF3-511) / Forschergruppe Gohlke $(hkf7_20170501)$},
      pid          = {G:(DE-HGF)POF3-511 / $G:(DE-Juel1)hkf7_20170501$},
      typ          = {PUB:(DE-HGF)16},
      pubmed       = {pmid:31762274},
      UT           = {WOS:000505633400020},
      doi          = {10.1021/acs.jmedchem.9b01489},
      url          = {https://juser.fz-juelich.de/record/867366},
}