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Stromyer ML , Southerland MR , Satyal U , Sikder RK , Weader DJ , Baughman JA , Youngs WJ , Abbosh PH
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
PMID: 31718944    PMCID: PMC7224591    URL: https://www.ncbi.nlm.nih.gov/pubmed/31718944
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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 250muM over a period of 1h 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.
1768-3254 Stromyer, Michael L Southerland, Marie R Satyal, Uttam Sikder, Rahmat K Weader, David J Baughman, Jessi A Youngs, Wiley J Abbosh, Philip H Journal Article France Eur J Med Chem. 2020 Jan 1;185:111832. doi: 10.1016/j.ejmech.2019.111832. Epub 2019 Oct 31.