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

[Display omitted] 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 (...

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Veröffentlicht in:	Bioorganic & medicinal chemistry letters 2016-05, Vol.26 (9), p.2142-2146
Hauptverfasser:	Gao, Ling-Jie, De Jonghe, Steven, Daelemans, Dirk, Herdewijn, Piet
Format:	Artikel
Sprache:	eng
Schlagworte:	Antineoplastic Agents - chemical synthesis Antineoplastic Agents - pharmacology Antitumoral Aspartic Acid - analogs & derivatives Aspartic Acid - chemical synthesis Aspartic Acid - pharmacology Cell Line, Tumor Drug Screening Assays, Antitumor Glutamates - chemical synthesis Glutamates - pharmacology Humans Nucleosides Nucleosides - chemical synthesis Nucleosides - pharmacology Organophosphorus Compounds - chemical synthesis Organophosphorus Compounds - pharmacology Prodrugs Prodrugs - chemical synthesis Prodrugs - pharmacology ProTides Structure-Activity Relationship
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Zusammenfassung:	[Display omitted] 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.
ISSN:	0960-894X 1464-3405
DOI:	10.1016/j.bmcl.2016.03.076