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@ARTICLE{Ortega:834832,
      author       = {Ortega, Jose Antonio and Arencibia, Jose M. and La Sala,
                      Giuseppina and Borgogno, Marco and Bauer, Inga and Bono,
                      Luca and Braccia, Clarissa and Armirotti, Andrea and
                      Girotto, Stefania and Ganesan, Anand and De Vivo, Marco},
      title        = {{P}harmacophore {I}dentification and {S}caffold
                      {E}xploration to {D}iscover {N}ovel, {P}otent, and
                      {C}hemically {S}table {I}nhibitors of {A}cid {C}eramidase in
                      {M}elanoma {C}ells},
      journal      = {Journal of medicinal chemistry},
      volume       = {60},
      number       = {13},
      issn         = {1520-4804},
      address      = {Washington, DC},
      publisher    = {ACS},
      reportid     = {FZJ-2017-04723},
      pages        = {5800 - 5815},
      year         = {2017},
      abstract     = {Acid ceramidase (AC) hydrolyzes ceramides, which are
                      central lipid messengers for metabolism and signaling of
                      sphingolipids. A growing body of evidence links deregulation
                      of sphingolipids to several diseases, including cancer.
                      Indeed, AC expression is abnormally high in melanoma cells.
                      AC inhibition may thus be key to treating malignant
                      melanoma. Here, we have used a systematic scaffold
                      exploration to design a general pharmacophore for AC
                      inhibition. This pharmacophore comprises a 6 + 5 fused ring
                      heterocycle linked to an aliphatic substituent via a urea
                      moiety. We have thus identified the novel benzimidazole
                      derivatives 10, 21, 27, and 30, which are highly potent AC
                      inhibitors. Their chemical and metabolic stabilities are
                      comparable or superior to those of previously reported AC
                      inhibitors. Moreover, they are potent against endogenous AC
                      in intact melanoma cells. These novel inhibitors merit
                      further characterization and can serve as a promising
                      starting point for the discovery of new antimelanoma
                      therapeutics.},
      cin          = {IAS-5 / INM-9},
      ddc          = {540},
      cid          = {I:(DE-Juel1)IAS-5-20120330 / I:(DE-Juel1)INM-9-20140121},
      pnm          = {899 - ohne Topic (POF3-899)},
      pid          = {G:(DE-HGF)POF3-899},
      typ          = {PUB:(DE-HGF)16},
      UT           = {WOS:000405764900035},
      pubmed       = {pmid:28603987},
      doi          = {10.1021/acs.jmedchem.7b00472},
      url          = {https://juser.fz-juelich.de/record/834832},
}