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Bioorg Med Chem Lett. 2016 May 1;26(9):2142-6. doi: 10.1016/j.bmcl.2016.03.076. Epub 2016 Mar 22.

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

Author information

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.

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

PMID:
27032331
DOI:
10.1016/j.bmcl.2016.03.076
[Indexed for MEDLINE]

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