{"database":"biostudies-literature","file_versions":[],"scores":null,"additional":{"submitter":["Farrell RE"],"funding":["Department of Education, Australian Government","Australian Institute of Nuclear Science and Engineering"],"pagination":["1973-1981"],"full_dataset_link":["https://www.ebi.ac.uk/biostudies/studies/S-EPMC11109934"],"repository":["biostudies-literature"],"omics_type":["Unknown"],"volume":["15(6)"],"pubmed_abstract":["Phosphonate and phosphate prodrugs are integral to enhancing drug permeability, but the potential toxicity of their metabolites requires careful consideration. This study evaluates the impact of widely used phosphoramidate, bis-amidate, and cycloSal phosph(on)ate prodrug metabolites on BxPC3 pancreatic cancer cells, GL261-Luc glioblastoma cells, and primary cultured mouse astrocytes. 1-Naphthol and 2-naphthol demonstrated the greatest toxicity. Notably, 2-naphthol exhibited an ED<sub>50</sub> of 21 μM on BxPC3 cells, surpassing 1-naphthol with an ED<sub>50</sub> of 82 μM. Real-time xCELLigence experiments revealed notable activity for both metabolites at a low concentration of 16 μM. On primary cultured mouse astrocyte cells, all prodrugs exhibited reduced viability at 128 to 256 μM after "],"journal":["RSC medicinal chemistry"],"pubmed_title":["Cytotoxicity of phosphoramidate, bis-amidate and cycloSal prodrug metabolites against tumour and normal cells."],"pmcid":["PMC11109934"],"funding_grant_id":["ALNSTU13115","ALNSTU12886"],"pubmed_authors":["Farrell RE","Middleton RJ","Liu GJ","Skropeta D","Steele H"],"additional_accession":[]},"is_claimable":false,"name":"Cytotoxicity of phosphoramidate, bis-amidate and cycloSal prodrug metabolites against tumour and normal cells.","description":"Phosphonate and phosphate prodrugs are integral to enhancing drug permeability, but the potential toxicity of their metabolites requires careful consideration. This study evaluates the impact of widely used phosphoramidate, bis-amidate, and cycloSal phosph(on)ate prodrug metabolites on BxPC3 pancreatic cancer cells, GL261-Luc glioblastoma cells, and primary cultured mouse astrocytes. 1-Naphthol and 2-naphthol demonstrated the greatest toxicity. Notably, 2-naphthol exhibited an ED<sub>50</sub> of 21 μM on BxPC3 cells, surpassing 1-naphthol with an ED<sub>50</sub> of 82 μM. Real-time xCELLigence experiments revealed notable activity for both metabolites at a low concentration of 16 μM. On primary cultured mouse astrocyte cells, all prodrugs exhibited reduced viability at 128 to 256 μM after ","dates":{"release":"2024-01-01T00:00:00Z","publication":"2024 Jun","modification":"2026-06-05T09:54:55.824Z","creation":"2025-08-18T09:52:59.232Z"},"accession":"S-EPMC11109934","cross_references":{"pubmed":["38903945"],"doi":["10.1039/d4md00115j"]}}