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      The design and cytotoxic evaluation of some 1-aryl-3-isopropylamino-1-propanone hydrochlorides towards human Huh-7 hepatoma cells

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      Author
      Mete, E.
      Gul, H. I.
      Cetin Atalay, R.
      Das, U.
      Sahin, E.
      Gul, M.
      Kazaz, C.
      Dimmock, J. R.
      Date
      2011
      Source Title
      Archiv der Pharmazie
      Print ISSN
      0365-6233
      Publisher
      Wiley
      Volume
      344
      Issue
      5
      Pages
      333 - 339
      Language
      English
      Type
      Article
      Item Usage Stats
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      Abstract
      A series of 1-aryl-3-isopropylamino-1-propanone hydrochlorides 1 and a related heterocyclic analog 2 as candidate antineoplastic agents were prepared and the rationale for designing these compounds is presented. A specific objective in this study is the discovery of novel compounds possessing growth-inhibiting properties of hepatoma cells. The compounds in series 1 and 2 were prepared and their structures established unequivocally. X-ray crystallography of two representative compounds 1d and 1g were achieved. Over half of the compounds are more potent than 5-fluorouracil which is an established drug used in treating liver cancers. QSAR evaluations and molecular modeling studies were undertaken with a view to detecting some physicochemical parameters which govern cytotoxic potencies. A number of guidelines for amplification of the project have been formulated. A number of Mannich bases displayed greater potency than the reference drug 5-fluorouracil against human Huh-7 hepatoma cells. In particular, 1i emerged as a lead compound possessing 2.8 fold higher activity than that of the reference drug. Copyright © 2011 WILEY-VCH Verlag GmbH & Co. KGaA, Weinheim.
      Keywords
      Anticancer drug design
      Huh-7 cells
      Mannich bases
      Molecular modeling
      QSAR
      Permalink
      http://hdl.handle.net/11693/21935
      Published Version (Please cite this version)
      http://dx.doi.org/10.1002/ardp.201000194
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