Design and synthesis of novel N(4)-substituted thiosemicarbazones bearing a pyrrole unit as potential anticancer agents

  • Authors:
    • Taofeng Zhu
    • Shanshan Shen
    • Qin Lu
    • Xingpei Ye
    • Weiliang Ding
    • Ruhua Chen
    • Jing Xie
    • Wenjiao Zhu
    • Jun Xu
    • Lei Jia
    • Weina Wu
    • Tieliang Ma
  • View Affiliations

  • Published online on: April 5, 2017     https://doi.org/10.3892/ol.2017.5995
  • Pages: 4493-4500
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Abstract

A series of N(4)-substituted thiosemicarbazones (TSCs) bearing pyrrole unit (1a‑1e) were synthesized and fully characterized by elemental analyses, infrared spectra, 1H nuclear magnetic resonance and single crystal X‑ray diffraction. The compounds were assessed as potential chemotherapeutic agents. All newly synthesized compounds were screened for their anticancer activity against lung cancer PC‑9, esophageal cancer Eca‑109 and gastric cancer SGC‑7901 cell lines. The results of MTT, Terminal deoxynucleotidyl transferase dUTP nick end labeling and fluorescence-activated cell sorting assays indicated that all the prepared compounds exhibited cytotoxicity against PC-9, Eca-109 and SGC-7901 cells in vitro. All the compounds significantly induced cancer cell apoptosis accompanied by increasing the Bax/Bcl‑2 ratio and activation of caspase‑3. The structure‑activity association was discussed and the potential pre‑clinical trials may be conducted. The present findings have a great potential in biomedical applications of novel N(4)‑substituted TSCs.
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June-2017
Volume 13 Issue 6

Print ISSN: 1792-1074
Online ISSN:1792-1082

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Spandidos Publications style
Zhu T, Shen S, Lu Q, Ye X, Ding W, Chen R, Xie J, Zhu W, Xu J, Jia L, Jia L, et al: Design and synthesis of novel N(4)-substituted thiosemicarbazones bearing a pyrrole unit as potential anticancer agents. Oncol Lett 13: 4493-4500, 2017.
APA
Zhu, T., Shen, S., Lu, Q., Ye, X., Ding, W., Chen, R. ... Ma, T. (2017). Design and synthesis of novel N(4)-substituted thiosemicarbazones bearing a pyrrole unit as potential anticancer agents. Oncology Letters, 13, 4493-4500. https://doi.org/10.3892/ol.2017.5995
MLA
Zhu, T., Shen, S., Lu, Q., Ye, X., Ding, W., Chen, R., Xie, J., Zhu, W., Xu, J., Jia, L., Wu, W., Ma, T."Design and synthesis of novel N(4)-substituted thiosemicarbazones bearing a pyrrole unit as potential anticancer agents". Oncology Letters 13.6 (2017): 4493-4500.
Chicago
Zhu, T., Shen, S., Lu, Q., Ye, X., Ding, W., Chen, R., Xie, J., Zhu, W., Xu, J., Jia, L., Wu, W., Ma, T."Design and synthesis of novel N(4)-substituted thiosemicarbazones bearing a pyrrole unit as potential anticancer agents". Oncology Letters 13, no. 6 (2017): 4493-4500. https://doi.org/10.3892/ol.2017.5995