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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},
}