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      • Department of Molecular Biology and Genetics
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      Synthesis and cytotoxic activity of novel 3-methyl-1-[(4-substitutedpiperazin-1-yl)methyl]-1 H-indole derivatives

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      Author
      Koksal, M.
      Yarim, M.
      Durmaz, I.
      Cetin Atalay, R.
      Date
      2012
      Source Title
      Arzneimittel-Forschung/Drug Research
      Print ISSN
      0004-4172
      Publisher
      Thieme
      Volume
      62
      Issue
      8
      Pages
      389 - 394
      Language
      English
      Type
      Article
      Item Usage Stats
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      125
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      Abstract
      A series of novel 3-methyl-1-[(4-substitutedpiperazin-1-yl)methyl]-1H- indoles (3a-l) were synthesized and their cytotoxicities were analyzed against 3 different human cell lines, including liver (HUH7), breast (MCF7) and colon (HCT116). The Mannich reaction of 3-methylindole (1) with 4- substitutedpiperazines (2) and formaldehyde resulted to the 3-methyl-1-[(4- substitutedpiperazin-1-yl)methyl]-1H-indoles (3a-l) in 38-69% yields. The investigation of anticancer screening revealed that the tested compounds showed comparable activity to the reference drug 5-fluorouracil and compounds 3g, 3h, 3i and 3k, had lower 50% inhibition (IC 50) concentration than reference drug. Moreover, the cytotoxic effect of the most potent compound 3h on HUH7 and MCF7 cells through apoptosis was visualized by Hoechst staining and compared with paclitaxel, which is a mitotic inhibitor acting on microtubules. The morphological features of apoptosis were observed as condensed and fragmented nuclei that are similar to paclitaxel. © Georg Thieme Verlag KG Stuttgart.New York.
      Keywords
      Anticancer
      Apoptosis
      Indole
      Mannich base
      Permalink
      http://hdl.handle.net/11693/21372
      Published Version (Please cite this version)
      http://dx.doi.org/10.1055/s-0032-1314868
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