Cyclo-saligenyl-5-fluoro-2′-deoxyuridinemonophosphate (cycloSal-FdUMP) — A New Prodrug Approach for FdUMP
- 1 July 1997
- journal article
- research article
- Published by Taylor & Francis in Nucleosides and Nucleotides
- Vol. 16 (7-9) , 1307-1310
- https://doi.org/10.1080/07328319708006177
Abstract
The synthesis of cycloSal-FdUMP 3a-d as a new prodrug approach for FdU 1 is described. Phosphotriesters 3 release the FdUMP 2 selectively by a controlled, chemically induced tandem reaction in hydrolysis studies. The biological activity (IC50) of cycloSal-phosphotriesters 3 was evaluated in FM3A/O cells and FM3A/TK− cells.Keywords
This publication has 4 references indexed in Scilit:
- 2‐Nucleos‐5′‐O‐yl‐4H‐1,3,2‐benzodioxaphosphinin‐2‐oxide—ein neues Konzept für lipophile, potentielle Prodrugs biologisch' aktiver NucleosidmonophosphateAngewandte Chemie, 1996
- Synthesis and Biological Evaluation of 5-Fluoro-2'-deoxyuridine Phosphoramidate AnalogsJournal of Medicinal Chemistry, 1995
- Synthesis and Antitumor Properties of Some Neutral Triesters of 5-Fluoro-2'-deoxyuridine-5'-monophosphate and 3',5'-Cyclic MonophosphateNucleosides, Nucleotides and Nucleic Acids, 1995
- 5'-[4-(Pivaloyloxy)-1,3,2-dioxaphosphorinan-2-yl]-2'-deoxy-5-fluorouridine: A Membrane-Permeating Prodrug of 5-Fluoro-2'-deoxyuridylic Acid (FdUMP)Journal of Medicinal Chemistry, 1995