Increased cellular proliferation is an integral part of the cancer phenotype. Hence, the sustained and continued demand on supply of DNA building blocks during the DNA replication presents a potential target for therapeutic intervention. For this propose, the α and Auger electron emitting nucleotides analogs are attractive for targeted endoradiotherapy, given that DNA of malignant cells is selectively addressed. This review summarizes development and preclinical and clinical studies of endoradiotherapeutic acting nucleoside analogs with a special focus on thymidine analogs.
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