Antiproliferative activity and mechanism of action of fatty acid derivatives of arabinofuranosylcytosine in leukemia and solid tumor cell lines.

@article{Bergman2004AntiproliferativeAA,
  title={Antiproliferative activity and mechanism of action of fatty acid derivatives of arabinofuranosylcytosine in leukemia and solid tumor cell lines.},
  author={Andries M. Bergman and Catharina M. Kuiper and Daphne Voorn and Elizabeth M. Comijn and Finn Myhren and Marit Liland Sandvold and Hans R. Hendriks and Godfridus J. Peters},
  journal={Biochemical pharmacology},
  year={2004},
  volume={67 3},
  pages={503-11}
}
1-beta-D-arabinofuranosylcytosine (ara-C) is a deoxycytidine analog with activity in leukemia, which requires phosphorylation by deoxycytidine kinase (dCK) to allow formation of its active phosphate 1-beta-D-arabinofuranosylcytosine triphosphate, but can be deaminated by deoxycytidine deaminase. Altered membrane transport is also a mechanism of drug resistance. In order to facilitate ara-C uptake and prolong retention in the cell, lipophilic prodrugs were synthesized. Fatty acid groups with a… CONTINUE READING
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