Novel bioconjugates of aminolevulinic acid with nucleosides
Author(s)
Gurba, Patrice
Vallinayagam, Ramakrishnan
Schmitt, Frederic
Furrer, Julien
Juillerat-Jeanneret, Lucienne
Date issued
2008
In
Synthesis
Vol
24
From page
3957
To page
3962
Subjects
Antitumor agents Esterification Human Neoplasm Prodrugs (prepn. and anticancer activity of aminolevulinic acid-nucleosides bioconjugates via esterification of nucleosides and aminolevulinic acid derivs.) Nucleosides Role: BPN (Biosynthetic preparation) PAC (Pharmacological activity) RCT (Reactant) SPN (Synthetic preparation) BIOL (Biological study) PREP (Preparation) RACT (Reactant or reagent) (prepn. and anticancer activity of aminolevulinic acid aminolevulinic acid nucleoside bioconjugate prepn esterification prodrug anticancer cancer human
Abstract
Esters and amino acid derivs. of 5-aminolevulinic acid (ALA) are efficient prodrugs for the prodn. of protoporphyrin IX (PpIX), which has been used in photodynamic cancer therapy (PDT). The synthesis of novel bioconjugates, e.g. I·CF3CO2H, combining ALA with adenosine and thymidine is reported. The novel bioconjugates have been made using a robust methodol. The new class of prodrugs contains one, two, or three ALA per mol. Preliminary cell tests in human cancer cell lines indicate that the thymidine conjugate of ALA is an efficient prodrug for PDT. [on SciFinder(R)]
Publication type
journal article