Nucleotide Chemotherapeutics – A Success Story Goes On!

The treatment of viral infectious diseases such as AIDS and Hepatitis C has witnessed spectacular progress in the recent past. By exploiting similar modes of pharmaceutical action (Scheme 1), various new nucleotide analogs (e.g. Tenofovir and Sofosbuvir) have been added to a growing list of antiviral and cytostatic drugs. It is our aim to provide you with antiviral and cytostatic nucleotide derivatives suitable for

• Pharmacodynamic approaches^[1,2]
• Lead structure identification^[3]
• Analytical standards^[4]

Scheme 1: Metabolism and pharmaceutical effects of antiviral and cytostatic nucleoside derivatives follow similar mechanisms^[5,6]. Nucleosides or their corresponding prodrugs enter the cytosol by active transport through the cell membrane where they undergo phosphorylation and/or further modification by cellular enzymes. The triphosphorylated products are incorporated into nucleic acids during replication or transcription, resulting in chain termination or mutagenesis.

Please refer to the following list of new lead compounds. In most cases custom-made derivatizations such as (poly)phosphorylation will be accessible.

Further Selected References

[5] Jordheim et al. (2013) Advances in the development of nucleoside and nucleotide analogues for cancer and viral diseases. Nat. Rev. Drug. Discov. 12 (6):447.
[6] Cavaliere et al. (2017) Fluorinated nucleosides as an important class of anticancer and antiviral agents. Future Med. Chem. 9 (15):1809.