nucleoside analog 1

Nucleoside-Analog-1 is a 4′-Azidocytidine analogue, used to against Hepatitis C virus replication.

1-Methylcytosine (4-amino-1-methylpyrimidin-2(1H)-one) is a methylated form of the cytosine and can be used as the nucleobase of hachimoji DNA paired with isoguanine.

AzddMeC (Az-Dcme) is a nucleoside analog with antiviral activity and is an orally active and selective inhibitor of HIV-1 reverse transcriptase and HIV-1 replication.AzddMeC has an EC50 value of 9 nM against HIV-1-infected human PBM cells and 6 nM against HIV-1-infected human macrophages.

Ganciclovir (2'-Nor-2'-deoxyguanosine) is an ACYCLOVIR analog that is a potent inhibitor of the Herpesvirus family including cytomegalovirus. Ganciclovir is used to treat complications from AIDS-associated cytomegalovirus infections.

Stavudine (BMY-27857), a nucleoside reverse transcriptase inhibitor analog of thymidine, has activity against HIV.

Acyclovir (Aciclovir) is a synthetic analog of the purine nucleoside, guanosine, with potent antiviral activity against herpes simplex viruses type 1 and 2, varicella-zoster virus and other viruses of the herpesvirus family.

Cytidine (Cytosine-1-β-D-ribofuranoside) is a pyrimidine nucleoside comprised of a cytosine bound to ribose via a beta-N1-glycosidic bond. Cytidine is a precursor for uridine. Both cytidine and uridine are utilized in RNA synthesis.

Ganciclovir sodium (Cytovene IV sodium) is the sodium salt of Ganciclovir with antiviral activity, especially against cytomegalovirus (CMV) and herpes simplex virus type 1 (HSV-1).

Tipiracil hydrochloride (MA-1 hydrochloride) is a thymidine phosphorylase inhibitor (TPI). Tipiracil hydrochloride is one of the active components in TAS-102, which is an anticancer drug candidate currently in clinical trials.

Efavirenz (DMP 266) is a Human Immunodeficiency Virus 1 Non-Nucleoside Analog Reverse Transcriptase Inhibitor, acting as a Non-Nucleoside Reverse Transcriptase Inhibitor, Cytochrome P450 3A Inducer, Cytochrome P450 2B6 Inducer, Cytochrome P450 2C9 Inhibitor, Cytochrome P450 2C19 Inhibitor, and Cytochrome P450 3A4 Inhibitor, classified as a Non-Nucleoside Analog.

EFdA-TP 3TEA is the salt form of EFdA-TP.EFdA-TP 3TEA is a nucleoside analog that is a novel, potent, and selective nucleoside reverse transcriptase (RT) inhibitor that inhibits HIV-1 reverse transcriptase by multiple mechanisms, thereby increasing its drug resistance.

Tizoxanide (Desacetyl-nitazoxanide) is a metabolite of lamivudine. Lamivudine (2', 3'-dideoxy-3'-thiacytidine, commonly called 3TC) is a potent nucleoside analog reverse transcriptase inhibitor (nRTI).

Ara-G is an analog of the nucleoside guanosine and an active metabolite of nelarabine .1,2 Ara-G accumulates in T lymphoblasts and malignant T-lymphoid cells, where it is phosphorylated to produce ara-GTP and incorporated into the DNA.3,1 Ara-G inhibits DNA replication by 92% after 30 minutes when used at a concentration of 50 μM in CEM cells, which are used as a model for human T lymphoblasts.1 It also halts the cell cycle at the sub-G1 phase and induces apoptosis in CEM cells.3 Syngeneic bone marrow containing 6C3HED tumor cells treated with ara-G (100 mM) ex vivo prior to transplantation increases survival of lethally irradiated mice and induces reconstitution of lymphoid, myeloid, and erythroid cell linages.4References1. Leanza, L., Miazzi, C., Ferraro, P., et al. Activation of guanine-β-D-arabinofuranoside and deoxyguanosine to triphosphates by a common pathway blocks T lymphoblasts at different checkpoints. Exp. Cell Res. 316(20), 3443-3453 (2010).2. Lambe, C.U., Averett, D.R., Paff, M.T., et al. 2-Amino-6-methoxypurine arabinoside: An agent for T-cell malignancies. Cancer Res. 55(15), 3352-3356 (1995).3. Rodriguez, C.O., Jr., Stellrecht, C.M., and Gandhi, V. Mechanisms for T-cell selective cytotoxicity of arabinosylguanine. Blood 102(5), 1842-1848 (2003).4. Kurtzberg, J. Guanine arabinoside as a bone marrow-purging agent. Ann. N.Y. Acad. Sci 685(1), 225-236 (1993). Ara-G is an analog of the nucleoside guanosine and an active metabolite of nelarabine .1,2 Ara-G accumulates in T lymphoblasts and malignant T-lymphoid cells, where it is phosphorylated to produce ara-GTP and incorporated into the DNA.3,1 Ara-G inhibits DNA replication by 92% after 30 minutes when used at a concentration of 50 μM in CEM cells, which are used as a model for human T lymphoblasts.1 It also halts the cell cycle at the sub-G1 phase and induces apoptosis in CEM cells.3 Syngeneic bone marrow containing 6C3HED tumor cells treated with ara-G (100 mM) ex vivo prior to transplantation increases survival of lethally irradiated mice and induces reconstitution of lymphoid, myeloid, and erythroid cell linages.4 References1. Leanza, L., Miazzi, C., Ferraro, P., et al. Activation of guanine-β-D-arabinofuranoside and deoxyguanosine to triphosphates by a common pathway blocks T lymphoblasts at different checkpoints. Exp. Cell Res. 316(20), 3443-3453 (2010).2. Lambe, C.U., Averett, D.R., Paff, M.T., et al. 2-Amino-6-methoxypurine arabinoside: An agent for T-cell malignancies. Cancer Res. 55(15), 3352-3356 (1995).3. Rodriguez, C.O., Jr., Stellrecht, C.M., and Gandhi, V. Mechanisms for T-cell selective cytotoxicity of arabinosylguanine. Blood 102(5), 1842-1848 (2003).4. Kurtzberg, J. Guanine arabinoside as a bone marrow-purging agent. Ann. N.Y. Acad. Sci 685(1), 225-236 (1993).

2',5-Difluoro-2'-deoxy-1-arabinosyluracil (2'-Deoxy-2'-fluoro-5-fluoro-arabinouridine) is a urinary pyrimidine nucleoside analogue with potential antiepileptic and antihypertensive activity, which can be used to study anticonvulsant and anxiety disorders.

SIBA (5'-Deoxy-5'-isobutylthioadenosine) is a synthetic analogue of SAH, acts as an inhibitor of S-adenosylmethionine-mediated transmethylation. SIBA can interfere with a variety of enzymatic activities in vitro, such as SAH hydrolase, methylthioadenosine phosphorylase and cAMP phosphodiesterase. SIBA reversibly blocks the multiplication of herpes simplex type 1 virus (HSV)

Gemcitabine-O-Si(di-iso)-O-Mc, a drug-linker conjugate for Antibody-Drug Conjugates (ADC), exhibits potent antitumor activity. It incorporates Gemcitabine, a pyrimidine nucleoside analog antimetabolite and antineoplastic agent, connected through the ADC linker [1].

1-Methylinosine (N1-Methylinosine) is a modified nucleotide found at position 37 in tRNA 3' to the anticodon of eukaryotic tRNA and has a role as a metabolite.

N1-Methylpseudouridine (1-Methylpseudouridine) is a methylpseudouridine and enhances translation through eIF2α-dependent and independent mechanisms by increasing ribosome density in mRNA.

Tenofovir exalidex (CMX 157) is a lipid-conjugated acyclic nucleotide analog of Tenofovir, demonstrating efficacy against wild-type and antiretroviral-resistant HIV strains, including those resistant to multiple nucleoside nucleotide analogs. It effectively inhibits all major HIV-1 and HIV-2 subtypes in fresh human PBMCs, as well as all evaluated HIV-1 strains in monocyte-derived macrophages, displaying EC50 values between 0.2 and 7.2 nM. Oral administration of CMX157 shows no apparent toxicity. Additionally, Tenofovir exalidex exhibits antiviral properties against HBV.

Censavudine (OBP-601) is a nucleoside analog, a nucleoside reverse transcriptase inhibitor, used for the prevention and treatment of human immunodeficiency virus 1 (HIV-1).Censavudine inhibits HIV-2 and HIV-1. Censavudine inhibits HIV-2 and HIV-1 with EC50 ranges of 30-81 nM and 450-890 nM, respectively.

GS-441524tris-isobutyryl ester is a prodrug form of the antiviral nucleoside analog and remdesivir metabolite GS-441524 .1It reduces the cytopathic effect of respiratory syncytial virus (RSV) in infected HEp-2 cells with an EC50value of 0.26 μM. 1.Mackman, R.L., Hui, H.C., Perron, M., et al.Prodrugs of a 1'-CN-4-aza-7,9-dideazaadenosine C-nucleoside leading to the discovery of remdesivir (GS-5734) as a potent inhibitor of respiratory syncytial virus with efficacy in the african green monkey model of RSVJ. Med. Chem.64(8)5001-5017(2021)

2'-Deoxy-2'-fluorocytidine, a nucleoside analog, is a potent inhibitor of Crimean-Congo hemorrhagic fever virus (CCHFV) replication and can act synergistically with T705 to enhance the antiviral effects on CCHFV replication[1]. It exhibits antiviral activity with EC50 values of 61 nM and 31 nM against CCHFV and CCHFV ZsG in Huh7 cells, respectively, and has a CC50 of >50.0 μM in Huh7 cells[1]. [1]. Stephen R Welch, et al. Identification of 2'-deoxy-2'-fluorocytidine as a potent inhibitor of Crimean-Congo hemorrhagic fever virus replication using a recombinant fluorescent reporter virus. Antiviral Res. 2017 Nov;147:91-99.

Ribavirin-13C5is intended for use as an internal standard for the quantification of ribavirin by GC- or LC-MS. Ribavirin is an antiviral guanosine nucleoside analog.1,2Upon entry into cells, ribavirin is metabolized to an active triphosphate form that induces viral RNA chain termination and inhibits viral polymerases. It reduces replication in a panel of seven RNA and four DNA viruses in Vero cells (EC50s = 2-95 μg/ml).3Ribavirin also reduces replication of severe acute respiratory syndrome coronavirus 2 (SARS-CoV-2) in Vero cells (EC50= 109.5 μM).4Aerosol administration of ribavirin (30 mg/kg) reduces mortality in a mouse model of influenza A infection.5Formulations containing ribavirin have been used in the treatment of respiratory syncytial virus (RSV), hepatitis C virus (HCV), and viral hemorrhagic fevers. 1.Gilbert, B.E., and Knight, V.Biochemistry and clinical applications of ribavirinAntimicrob. Agents Chemother.30(2)201-205(1986) 2.Gordon, C.J., Tchesnokov, E.P., Woolner, E., et al.Remdesivir is a direct-acting antiviral that inhibits RNA-dependent RNA polymerase from severe acute respiratory syndrome coronavirus 2 with high potencyJ. Biol. Chem.295(20)6785-6797(2020) 3.Kirsi, J.J., North, J.A., McKernan, P.A., et al.Broad-spectrum antiviral activity of 2-β-D-ribofuranosylselenazole-4-carboxamide, a new antiviral agentAntimicrob. Agents Chemother.24(3)353-361(1983) 4.Wang, M., Cao, R., Zhang, L., et al.Remdesivir and chloroquine effectively inhibit the recently emerged novel coronavirus (2019-nCoV) in vitroCell Res.30(3)269-271(2020) 5.Wilson, S.Z., Knight, V., Wyde, P.R., et al.Amantadine and ribavirin aerosol treatment of influenza A and B infection in miceAntimicrob. Agents Chemother.17(4)642-648(1980)

Antiviral agent 17 (Compound 4) is an anti-infection compound with strong antiviral effects, demonstrated by an EC50 of 0.015 μM in a human replicon assay, and effective against murine norovirus. It has potential applications in studying infectious and malignant diseases[1].