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      • Department of Molecular Biology and Genetics
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      Synthesis and preliminary mechanistic evaluation of 5-(p-tolyl)-1-(quinolin-2-yl)pyrazole-3-carboxylic acid amides with potent antiproliferative activity on human cancer cell lines

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      Author(s)
      Cankara-Pirol, Ş.
      Çalışkan, B.
      Durmaz, İrem
      Atalay, Rengül
      Banoğlu, E.
      Date
      2014
      Source Title
      European Journal of Medicinal Chemistry
      Print ISSN
      0223-5234
      Publisher
      Elsevier
      Volume
      87
      Pages
      140 - 149
      Language
      English
      Type
      Article
      Item Usage Stats
      310
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      335
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      Abstract
      We synthesized a series of novel amide derivatives of 5-(p-tolyl)-1-(quinolin-2-yl)pyrazole-3-carboxylic acid and assessed their antiproliferative activities against three human cancer cell lines (Huh7, human liver; MCF7, breast and HCT116, colon carcinoma cell lines) with the sulforhodamine B assay. Compound 4j with 2-chloro-4-pyridinyl group in the amide part exhibited promising cytotoxic activity against all cell lines with IC<inf>50</inf>values of 1.6 μM, 3.3 μM and 1.1 μM for Huh7, MCF7 and HCT116 cells, respectively, and produced dramatic cell cycle arrest at SubG1/G1 phase as an indicator of apoptotic cell death induction. On the basis of their high potency in cellular environment, these straightforward pyrazole-3-carboxamide derivatives may possess potential in the design of more potent compounds for intervention with cancer cell proliferation.
      Keywords
      Apoptosis
      Autophagy
      Cytotoxicity
      Diarylpyrazole
      Quinoline
      G1 phase
      Permalink
      http://hdl.handle.net/11693/24936
      Published Version (Please cite this version)
      https://doi.org/10.1016/j.ejmech.2014.09.056
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      • Department of Molecular Biology and Genetics 542
      • Genetics and Biotechnology Research Center (BİLGEN) 16
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