Nucléosides

Inhibitor of reverse transcriptase

Abacavir is a carbocyclic 2'-deoxyguanosine nucleoside reverse transcriptase (RT) inhibitor with anti-retroviral activity against HIV. Good oral bioavailability, high aqueous solubility and good cerebrospinal fluid penetrance. Synergistic with other nucleoside RT inhibitors such as AZT.

Tenofovir is an acyclic nucleoside phosphonate that exhibits anti-viral properties through its inhibition of reverse transcriptases. In particular, Tenofovir is a potent inhibitor of Human Immunodeficiency Virus (HIV) and chronic Hepatitis B Virus (HBV) reverse transcriptases, thus preventing the replication of genetic viral material. This property is beneficial in virus research areas and developing antiviral treatments. Once inside the body tenofovir is metabolized into its active form, tenofovir diphosphate, by the lysosomal protease cathepsin A, nucleotide kinases and adenylate kinases. An oral prodrug, used in the treatment of HIV, is tenofovir alafenamide (TAF) hemifumerate and this has improved stability, greater antiviral activity and reduces the risk of side effects such as loss of kidney function. Furthermore, TAF is easily metabolized into tenofovir in the lymphocytes allowing increased drug accumulation in HIV cells.

Anti-viral; reverse transcriptase inhibitor

Anti-viral; anti-neoplastic

Ribonuclesides are a class of modified nucleosides that have been shown to be effective against cancer cells. Oleoyl CoA potassium salt is a Ribonucleoside that inhibits the growth of cancer cells by inhibiting DNA synthesis and RNA synthesis. The Ribonucleosides inhibit the formation of DNA by preventing the conversion of ribose-5-phosphate to deoxyribose-5-phosphate, which is required for DNA synthesis. Oleoyl CoA potassium salt also binds to the enzyme ribonucleotide reductase, which converts ribonucleotides into deoxyribonucleotides, thereby inhibiting DNA synthesis. This drug has been studied in preclinical animal trials.

Based functionalised uridine

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5'-O-DMT-uridine is an oligodeoxynucleotide that has been conjugated to tetracycline. It is a bioconjugate that can be used for photooxidation of DNA, as well as for the prevention of bacterial efflux. The 5'-O-DMT group can be removed from the uridine by light irradiation or by bioconjugate chemistry, which results in the release of tetracycline and subsequent binding to bacterial ribosomes. This prevents protein synthesis and cell division. The linker can be any cyclic or dehydrating compound.

Inhibition of decapping.

2-Fluoro-6-O-[2-(4-nitrophenyl)ethyl]inosine (2F-6ENPE) is a novel antiviral agent that inhibits the synthesis of RNA in the body. It is a monophosphate nucleotide analog and a prodrug that is converted to its active form, 2F-6ENP by ribonucleoside kinases. This drug has been shown to inhibit the growth of cancer cells in vitro and in vivo. 2F-6ENPE has also been shown to be effective against methicillin resistant staphylococcus aureus (MRSA).

8-Chloro-2'-deoxyadenosine is a nucleoside analogue and a disinfectant that inhibits the synthesis of DNA. It has been used to control active viruses and to induce apoptotic cell death in cancer cells. 8-Chloro-2'-deoxyadenosine binds to viral RNA and DNA, preventing viral replication by inhibiting the activity of reverse transcriptase, which is an enzyme that copies the virus's genetic information from RNA into DNA. This drug has also been shown to be effective for the treatment of HIV infection. 8-Chloro-2'-deoxyadenosine disrupts DNA synthesis and cellular metabolism by blocking transcription and protein synthesis.

2'-Deoxyadenosine 5'-O-thiophosphate sodium salt is a synthetic nucleotide that has antiviral, anticancer and antitumor properties. It is a modified deoxyribonucleoside and it activates the synthesis of DNA by acting as an activator. This drug is not found in nature and it has shown to inhibit the growth of human breast cancer cells in cell culture.

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2'-O-Me protected nucleoside