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.
- 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: [email protected].
- 5. Molecular Therapeutics Program, Fox Chase Cancer Center, 333 Cottman Avenue, Philadelphia, PA, 19111, USA. Electronic address: [email protected].
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.
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