A Diazirine-based Nucleoside Analogue For Efficient Dna Interstrandrnphotocross-linking

摘要

A common strategy for cancer therapy is to induce DNA damage and subsequent apoptosis of cancer cells. Some of the most effective anticancer agents in clinical use, such as cyclophosphamide, mitomycin C, and cisplatin, exert their effects by creating DNA interstrand cross-links. We report here the design and synthesis of a diazirine-based nucleoside analogue (DBN, Figure 1) that can be incorporated into DNA by solid phase oligonucleotide synthesis. The DBN-containing dsDNA efficiently forms an interstranded cross-link upon photoirradiation.