2. Academic Validation
  3. Synthesis and anti-proliferative activity of fluoro-substituted chalcones

Synthesis and anti-proliferative activity of fluoro-substituted chalcones

  • Bioorg Med Chem Lett. 2016 Jul 1;26(13):3172-3176. doi: 10.1016/j.bmcl.2016.04.096.
Serdar Burmaoglu 1,  Oztekin Algul 2,  Derya Aktas Anıl 3,  Arzu Gobek 3,  Gulay Gulbol Duran 4,  Ronak Haj Ersan 5,  Nizami Duran 6
Affiliations

Affiliations

  • 1 Tercan Vocational High School, Erzincan University, Erzincan 24800, Turkey; Department of Chemistry, Faculty of Science, Ataturk University, Erzurum 25240, Turkey. Electronic address: [email protected].
  • 2 Department of Pharmaceutical Chemistry, Faculty of Pharmacy, Mersin University, Mersin 33169, Turkey. Electronic address: [email protected].
  • 3 Department of Chemistry, Faculty of Science, Ataturk University, Erzurum 25240, Turkey.
  • 4 Department of Medical Biology, Medical Faculty, Mustafa Kemal University, Antakya-Hatay 31100, Turkey.
  • 5 Department of Pharmaceutical Chemistry, Faculty of Pharmacy, Mersin University, Mersin 33169, Turkey.
  • 6 Department of Medical Microbiology, Medical Faculty, Mustafa Kemal University, Antakya-Hatay 31100, Turkey.
PMID: 27217001 DOI: 10.1016/j.bmcl.2016.04.096
Abstract

A series of novel fluoro-substituted chalcone derivatives have been synthesized. All synthesized compounds were characterized by (1)H nuclear magnetic resonance (NMR), (13)C NMR, and elemental analysis. Their anti-proliferative activities were evaluated against five Cancer cells lines, namely, A549, A498, HeLa, A375, and HepG2 using the MTT method. Most of the compounds showed moderate to high activity with IC50 values in the range of 0.029-0.729μM. Of all the synthesized compounds, 10 and 19 exhibited the most potent anti-proliferative activities against Cancer cells, and 10 was identified as the most promising compound.

Keywords

Anti-proliferative activity; Chalcone; Claisen–Schmidt condensation; Organofluorine; Synthesis.

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