2. Academic Validation
  3. L-Aspartic and l-glutamic acid ester-based ProTides of anticancer nucleosides: Synthesis and antitumoral evaluation

L-Aspartic and l-glutamic acid ester-based ProTides of anticancer nucleosides: Synthesis and antitumoral evaluation

  • Bioorg Med Chem Lett. 2016 May 1;26(9):2142-6. doi: 10.1016/j.bmcl.2016.03.076.
Ling-Jie Gao 1,  Steven De Jonghe 1,  Dirk Daelemans 2,  Piet Herdewijn 3
Affiliations

Affiliations

  • 1 KU Leuven, Rega Institute for Medical Research, Laboratory of Medicinal Chemistry, Minderbroedersstraat 10, 3000 Leuven, Belgium.
  • 2 KU Leuven, Rega Institute for Medical Research, Laboratory of Virology and Chemotherapy, Minderbroedersstraat 10, 3000 Leuven, Belgium.
  • 3 KU Leuven, Rega Institute for Medical Research, Laboratory of Medicinal Chemistry, Minderbroedersstraat 10, 3000 Leuven, Belgium. Electronic address: piet.herdewijn@kuleuven.be.
PMID: 27032331 DOI: 10.1016/j.bmcl.2016.03.076
Abstract

A series of novel aryloxyphosphoramidate nucleoside prodrugs based on l-aspartic acid and l-glutamic acid as amino acid motif has been synthesized and evaluated for antitumoral activity. Depending on the Cancer cell line studied and on the nature of the parent nucleoside compound (gemcitabine, 5-iodo-2'-deoxy-uridine, floxuridine or brivudin), the corresponding ProTides are endowed with an improved or decreased cytotoxic activity.

Keywords

Antitumoral; Nucleosides; ProTides; Prodrugs.

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