% IMPORTANT: The following is UTF-8 encoded.  This means that in the presence
% of non-ASCII characters, it will not work with BibTeX 0.99 or older.
% Instead, you should use an up-to-date BibTeX implementation like “bibtex8” or
% “biber”.

@ARTICLE{Chen:282518,
      author       = {X. Chen and J. Wang and P. Zhao and B. Dang and T. Liang
                      and R. Steimbach$^*$ and A. Miller$^*$ and J. Liu and X.
                      Wang and T. Zhang and X. Luan and J. Hu and J. Gao},
      title        = {{T}etrahydro-β-carboline derivatives as potent histone
                      deacetylase 6 inhibitors with broad-spectrum
                      antiproliferative activity.},
      journal      = {European journal of medicinal chemistry},
      volume       = {260},
      issn         = {0009-4374},
      address      = {Amsterdam [u.a.]},
      publisher    = {Elsevier Science},
      reportid     = {DKFZ-2023-01807},
      pages        = {115776},
      year         = {2023},
      abstract     = {A series of tetrahydro-β-carboline (THβC)-based
                      hydroxamic acids were rationally designed and synthesized as
                      novel selective HDAC6 inhibitors (sHDAC6is) by the
                      application of scaffold hopping strategy. Several THβC
                      analogues were highly potent (IC50 < 5 nM) and selective
                      against HDAC6 enzyme and exhibited good antiproliferative
                      activity against human multiple myeloma (MM) cell. Molecular
                      docking interpreted the structure activity relationship
                      (SAR). Target engagement of HDAC6 was confirmed in RPMI-8226
                      cells using the WB assay. In vitro, (1S,
                      3R)-1-(4-chlorophenyl)-N-(4-(hydroxycarbamoyl)benzyl)-2,3,4,9-tetrahydro-1H-pyrido[3,
                      4-b]indole-3-carboxamide (14g) showed potent broad
                      antiproliferative activity against various tumors including
                      leukemia, colon cancer, melanoma, and breast cancer cell
                      lines, better than ACY-1215. Moreover, 14g also showed good
                      pharmacokinetics properties in mice via oral
                      administration.},
      keywords     = {Antiproliferative (Other) / HDAC6 inhibitor (Other) /
                      Selectivity (Other) / Synthesis (Other) / THβC (Other)},
      cin          = {A390 / HD01},
      ddc          = {610},
      cid          = {I:(DE-He78)A390-20160331 / I:(DE-He78)HD01-20160331},
      pnm          = {311 - Zellbiologie und Tumorbiologie (POF4-311)},
      pid          = {G:(DE-HGF)POF4-311},
      typ          = {PUB:(DE-HGF)16},
      pubmed       = {pmid:37660484},
      doi          = {10.1016/j.ejmech.2023.115776},
      url          = {https://inrepo02.dkfz.de/record/282518},
}