Interference with DNA replication affects rapidly proliferating cancer cells preferentially, which has prompted us to design and synthesize potential anti-cancer agents capable of halting DNA synthesis. The hypothetical mechanism of action of our base-modified nucleoside drug candidates is their intracellular metabolism into 5'-triphosphates whose subsequent incorporation into DNA replication fork obstructs further addition of nucleotides. In order to support the hypothesis, we have synthesized fluorescent dye labeled drug candidates, compared their activity to that of the unlabeled analog, and examined their cellular uptake and distribution using confocal microscopy.

Fluorescent dye-labeled novel anticancer drug candidates: Cellular uptake and distribution studies

247th National Meeting (2014)

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