Telomerase inhibition by 3′-azido-2′, 3′-dideoxynucleoside 5′-triphosphates and telomere shortening in human cultured cells by the corresponding nucleosides

Abstract

Telomerase is believed to be a good target for the development of antitumor agents. In this study, 3′-azido-2′,3′-dideoxy-2-aminoadenosine (AZddAA), 3′-azido-2′,3′-dideoxyadenosine (AZddA), 9-(3-azido-2,3-dideoxy-β-D-ribofuranosyl)-2-aminopurine (AZddAP), 3′-azido-2-chloro-2′,3′-dideoxyadenosine (AZddClA) and their triphosphate derivatives were synthesized. Telomerase assay studies showed that the 2-amino group plays an important role in the inhibitory activity of these compounds. In addition, AZddAA was found to cause telomere shortening in of HL60 cells in culture.

Author notes

1Department of Biosciences, Teikyo University of Science and Technology, Uenohara, Yamanashi 409-0193, Japan, 2Biotechnology Research Center, Teikyo University of Science and Technology, Uenohara, Yamanashi 409-0193, Japan