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Makale Tam Makale Uluslararası 2016

Synthesis and bioactivity studies of 1-aryl-3-(2-hydroxyethylthio)-1-propanones

Elif UNLUER, Halise İnci Gül, Alkan DEMIRTAS, Hiroshi SAKAGAMI, Naoki UMEMURA, Muhammet TANC, Cavit Kazaz, Claudiu T. SUPURAN

JOURNAL OF ENZYME INHIBITION AND MEDICINAL CHEMISTRY Cilt 31 · ss. 105–109 · 01.12.2016
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Özet

A series of Mannich bases having piperidine moiety were reacted with 2-mercaptoethanol, leading to 1-aryl-3-piperidine-4-yl-1-propanone hydrochlorides. The cytotoxicity and carbonic anhydrase inhibitory activities of these new compounds were evaluated. Among the compounds, only one derivative, nitro substituent bearing EU9, showed an effective cytotoxicity, although weak tumor specificity against human oral malignant versus nonmalignant cells. The compound induced apoptosis in HSC-2 oral squamous cell carcinoma cells, but not in human gingival fibroblast. Chemical modifications of this lead are thus necessary to further investigate it as a drug candidate and to obtain compounds with a better activity profile.

Anahtar kelimeler

cytotoxicity DNA TOPOISOMERASE-I JURKAT CELLS HYDROCHLORIDES CARBONIC-ANHYDRASE INHIBITORS BIS MANNICH-BASES CORRESPONDING AZINE DERIVATIVES piperidinols CELLULAR GLUTATHIONE CANCER CELLS CARBONIC-ANHYDRASE INHIBITION PARP thiol addition

Atıf için künye

UNLUER, E., Gül, H. İ., DEMIRTAS, A., SAKAGAMI, H., UMEMURA, N., TANC, M., Kazaz, C., & SUPURAN, C. T. (2016). Synthesis and bioactivity studies of 1-aryl-3-(2-hydroxyethylthio)-1-propanones. JOURNAL OF ENZYME INHIBITION AND MEDICINAL CHEMISTRY, 31, 105–109. https://doi.org/10.1080/14756366.2016.1209495

BibTeX 
@article{unluer2016-19956,
  author = {UNLUER, Elif and Gül, Halise İnci and DEMIRTAS, Alkan and SAKAGAMI, Hiroshi and UMEMURA, Naoki and TANC, Muhammet and Kazaz, Cavit and SUPURAN, Claudiu T.},
  title = {Synthesis and bioactivity studies of 1-aryl-3-(2-hydroxyethylthio)-1-propanones},
  journal = {JOURNAL OF ENZYME INHIBITION AND MEDICINAL CHEMISTRY},
  year = {2016},
  volume = {31},
  pages = {105--109},
  issn = {1475-6366},
  doi = {10.1080/14756366.2016.1209495},
  url = {https://akademik.atauni.edu.tr/yayinlar/19956-synthesis-and-bioactivity-studies-of-1-aryl-3-2-hydroxyethylthio-1-propanones}
}