EICAR is a drug which acts as an inhibitor of the enzyme IMP dehydrogenase. It is a nucleoside derivative which has both anti-cancer and antiviral effects, and was originally developed for the treatment of leukemia, but was unsuccessful in human clinical trials. It has broad spectrum antiviral effects with activity against vaccinia virus, Semliki forest virus, Junin virus, reovirus, influenza, measles virus and respiratory syncytial virus among others, although it is not active against SARS. This useful spectrum of activity means that EICAR and related derivatives continue to be investigated for the treatment of viral diseases.
5'-Ethynyl-2'-deoxycytidine (EdC) functions as a nucleoside analog effectively inhibiting the replication of herpes simplex virus-1 (HSV-1) KOS strain with an ID50 of 0.2 μg/mL. Additionally, it decreases virus-induced cytopathogenic effects in PRK cells for HSV-1, HSV-2, and vaccinia virus strains, demonstrating MIC values between 0.2 to 5 μg/mL. EdC acts as a thymidylate synthetase inhibitor, selectively impacting the DNA incorporation rates of [1',2'-3H]deoxyuridine compared to [CH3-3H]deoxythymidine in PRK cells with ID50s of 3 and 120 μg/mL, respectively. It further inhibits thymidine synthetase and curtails L1210 cell proliferation, a process reversible by deoxythymidine (ID50s are 4.4 and 1,000 μg/mL, respectively). Also, EdC is utilized in monitoring DNA synthesis and cellular replication through click chemistry conjugation, linking its ethynyl group with the azido group of various fluorochromes.