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      Synthesis of 3-aroyl-4-aryl-1-isopropylamino-4-piperidinols and evaluation of the cytotoxicities of the compounds against human hepatoma and breast cancer cell lines

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      Author
      Kucukoglu, K.
      Mete, E.
      Cetin-Atalay, R.
      Gul H.I.
      Date
      2015
      Source Title
      Journal of Enzyme Inhibition and Medicinal Chemistry
      Print ISSN
      14756366
      Publisher
      Taylor and Francis Ltd
      Volume
      30
      Issue
      4
      Pages
      564 - 568
      Language
      English
      Type
      Article
      Item Usage Stats
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      Abstract
      Some 4-piperidinol derivatives were synthesized and their cytotoxicity was tested against human hepatoma (Huh7) and breast cancer (T47D) cells. Aryl part was changed as phenyl in 2a, 4-methylphenyl in 2b, 4-methoxyphenyl in 2c, 4-chlorophenyl in 2d, 4-fluorophenyl in 2e, 4-bromophenyl in 2f, 4-nitrophenyl in 2g and 2-thienyl in 3. Compounds were synthesized and reported for the first time by this study except 2a and 2d. Chemical structures were confirmed by 1H NMR, 13C NMR, IR, MS and elemental analyses. Compounds 2a (3.1 times), 2c (3.8 times), 2f (4.6 times), 2g (1.3 times) and 3 (3.2 times) had 1.3-4.6 times higher cytotoxic potency than the reference compound 5-FU against Huh7 cell line while all the compounds synthesized had shown lower activities against T47D cell line than 5-FU. In the light of these results, compounds 2a, 2c, 2f, 2g and 3 may serve as model compounds for further studies. © 2014 Informa UK Ltd.
      Keywords
      Cytotoxicity
      Huh7 cells
      isopropylamine
      Mannich bases
      T47D cells
      2 thienyl
      3 aroyl 4 aryl 1 isopropylamino 4 piperidinol derivative
      4 bromophenyl
      4 chlorophenyl
      4 fluorophenyl
      4 methoxyphenyl
      4 methylphenyl
      4 nitrophenyl
      antineoplastic agent
      fluorouracil
      unclassified drug
      antineoplastic activity
      Article
      breast cancer cell line
      carbon nuclear magnetic resonance
      cytotoxicity
      drug synthesis
      human
      human cell
      infrared spectroscopy
      liver cancer cell line
      mass spectrometry
      priority journal
      proton nuclear magnetic resonance
      Permalink
      http://hdl.handle.net/11693/21425
      Published Version (Please cite this version)
      http://dx.doi.org/10.3109/14756366.2014.951350
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