Fully automated high-performance liquid chromatographic method for the determination of carzelesin (U-80,244) and metabolites (U-76,073 and U-76,074) in human plasma.

@article{Tellingen1994FullyAH,
  title={Fully automated high-performance liquid chromatographic method for the determination of carzelesin (U-80,244) and metabolites (U-76,073 and U-76,074) in human plasma.},
  author={Olaf van Tellingen and Elżbieta Pels and Roland E. C. Henrar and Larry J. Schaaf and Guy E. Padbury and Jos H. Beijnen and Willem J. Nooijen},
  journal={Journal of chromatography},
  year={1994},
  volume={652 1},
  pages={
          51-8
        }
}
Carzelesin (U80,244, I) is a cyclopropylpyrroloindole prodrug analog. The compound exerts its cytotoxic activity after conversion, via U-76,073 (II) to U-76,074 (III) by binding to the DNA minor groove in a sequence selective fashion. In pre-clinical investigations the drug displayed a broad spectrum activity against human xenografts in mice. To enable pharmacokinetic monitoring during the phase I clinical trials, we have developed a selective and sensitive assay for the parent compound and its… CONTINUE READING
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