PARP inhibitor cyanine dye conjugate with enhanced cytotoxic and antiproliferative activity in patient derived glioblastoma cell lines.
作者： Peter J Choi , Elizabeth Cooper , Patrick Schweder , Edward Mee , Clinton Turner
DOI: 10.1016/J.BMCL.2020.127252
关键词:
摘要: Abstract We describe the synthesis and in vitro activity of drug-dye conjugate 1, which is a combination PARP inhibitor rucaparib heptamethine cyanine dye IR-786. The 1 was evaluated three different patient-derived glioblastoma cell lines showed strong cytotoxic with nanomolar potency (EC50: 128 nM), 780 fold improvement over itself. also observe synergistic effect temozolomide (TMZ), standard drug for treatment even though these were resistant to TMZ treatment. envisage such conjugates be worth exploring their utility various brain cancers.
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