2. Academic Validation
  3. Synthesis, characterization, and biological activity of a triphenylphosphonium-containing imidazolium salt against select bladder cancer cell lines

Synthesis, characterization, and biological activity of a triphenylphosphonium-containing imidazolium salt against select bladder cancer cell lines

  • Eur J Med Chem. 2020 Jan 1;185:111832. doi: 10.1016/j.ejmech.2019.111832.
Michael L Stromyer 1,  Marie R Southerland 1,  Uttam Satyal 2,  Rahmat K Sikder 2,  David J Weader 3,  Jessi A Baughman 1,  Wiley J Youngs 4,  Philip H Abbosh 5
Affiliations

Affiliations

  • 1 Department of Chemistry, The University of Akron, 190 East Buchtel Commons, Akron, OH, 44325, USA.
  • 2 Molecular Therapeutics Program, Fox Chase Cancer Center, 333 Cottman Avenue, Philadelphia, PA, 19111, USA.
  • 3 Department of Chemistry, The University of Akron, 190 East Buchtel Commons, Akron, OH, 44325, USA; Molecular Therapeutics Program, Fox Chase Cancer Center, 333 Cottman Avenue, Philadelphia, PA, 19111, USA.
  • 4 Department of Chemistry, The University of Akron, 190 East Buchtel Commons, Akron, OH, 44325, USA. Electronic address: Youngs@uakron.edu.
  • 5 Molecular Therapeutics Program, Fox Chase Cancer Center, 333 Cottman Avenue, Philadelphia, PA, 19111, USA. Electronic address: Philip.abbosh@fccc.edu.
PMID: 31718944 DOI: 10.1016/j.ejmech.2019.111832
Abstract

Imidazolium salts have shown great promise as Anticancer materials. A new imidazolium salt (TPP1), with a triphenylphosphonium substituent, has been synthesized and evaluated for in vitro and in vivo cytotoxicity against bladder Cancer. TPP1 was determined to have a GI50 ranging from 200 to 250 μM over a period of 1 h and the ability to effectively inhibit bladder Cancer. TPP1 induces Apoptosis, and it appears to act as a direct mitochondrial toxin. TPP1 was applied intravesically to a bladder Cancer mouse model based on the carcinogen N-butyl-N-(4-hydroxybutyl)nitrosamine (BBN). Cancer selectivity of TPP1 was demonstrated, as BBN-induced tumors exhibited Apoptosis but normal adjacent urothelium did not. These results suggest that TPP1 may be a promising intravesical agent for the treatment of bladder Cancer.

Keywords

Apoptosis; Bladder cancer; Imidazolium salt; Triphenylphosphonium salt.

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