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Novel bioconjugates of aminolevulinic acid with nucleosides

2008, Gurba, Patrice, Vallinayagam, Ramakrishnan, Schmitt, Frederic, Furrer, Julien, Juillerat-Jeanneret, Lucienne, Neier, Reinhard

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)]