Sucres du squelette et nucléobases

6-Cyanopurine is an antiviral agent that is a structural analog of adenine. The compound has been shown to inhibit the growth of murine sarcoma virus and herpes simplex virus, while also inhibiting the synthesis of bacterial DNA. 6-Cyanopurine inhibits bacterial growth by binding to the enzyme aldehyde oxidase, which is required for the production of cellular energy in mitochondria. This binding prevents the formation of ATP, which is required for replication and transcription in bacteria. In addition, 6-Cyanopurine may also have antimicrobial activity against tuberculosis and other infections caused by intracellular bacteria. 6-Cyanopurine binds to phosphonates and imidazoles and inhibits their regulatory function on bacterial growth.

9-Ethylguanine is a protonated guanine derivative that has significant cytotoxicity. It is an analog of the natural nucleobase guanosine and is structurally similar to the group P2 purine base, hypoxanthine. 9-Ethylguanine specifically binds with nitrogen atoms in DNA, forming hydrogen bonds with adjacent bases. The compound has low potency and therefore must be administered at high doses for it to be effective. 9-Ethylguanine has been shown to have anticancer activity against cervical cancer cells in cell cultures, but no biological studies have been conducted on other cancer types.

Cy7-YNE is a fluorescence labeling agent (Ex=700-770 nm,Em=790 nm) used for labeling antibodies, proteins, and peptides.

5-O-Carboranyl-1-(2-Deoxy-2-Fluoro-beta-D-Arabinofuranosyl)Uracil is a cell culture reagent that can be used to study the physicochemical properties of HIV. It has been shown to inhibit human immunodeficiency virus (HIV) infection of both CD4+ and CD8+ T cells in the laboratory. This compound also inhibits herpes simplex virus type 1 (HSV1) replication, which may be due to its ability to act as a sensitizer and modify the viral protein capsid. 5-O-Carboranyl-1-(2-Deoxy-2-Fluoro-beta-D-Arabinofuranosyl)Uracil has been shown to have pharmaceutical properties that are beneficial in treating human gliomas and other cancers.

2-Thiouracil is a photochemical that reacts with DNA by intermolecular hydrogen bonding, leading to DNA strand breakage. The reaction mechanism of 2-thiouracil has been elucidated through in vitro assays, which showed that the drug binds to the major groove of DNA duplexes and causes cleavage in the region containing two nitrogen atoms.

Sulfo-Cy5.5 is a near-infrared fluorescent dye that can be used to label biomolecules such as peptides, proteins, and oligonucleotides [2].

6-Benzylamino-7-deazapurine is a drug that has been shown to be effective in the treatment of pancreatic cancer. It is a monomer that reacts with nucleophiles such as 6-mercaptopurine, which are present in the human lung. The reaction generates an exergonic molecule that can be used to generate ATP and regenerate NAD+ during irradiation. This process has been observed using kinetic studies on human colon adenocarcinoma cells. 6-Benzylamino-7-deazapurine can also react with triazole compounds to form a linker and increase the rate of polymerization. The optimization of this reaction time could lead to more efficient cancer treatments.

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3-(2-Tetrahydrofuryl)-5-fluorouracil (3HFTU) is a fluorinated analog of 5-fluorouracil, a drug used in the clinical treatment of cancer. 3HFTU is used as an adjuvant therapy to increase the uptake and inhibitory properties of 5-fluorouracil in tumor tissue. This compound has been shown to be effective in inhibiting the growth of tumors by reducing their size and spread. 3HFTU has also been shown to have inhibitory properties against DNA synthesis, RNA synthesis, and protein synthesis. The chemical ionization technique is used to measure the diameter of 3HFTU particles. 3HFTU samples are prepared for measurement by adding a solvent that dissolves all solids and then filtering away the solids. A clinical use for this product is to provide adjuvant therapy for patients with cancerous tumors, who are undergoing radiation therapy or

O,O'-Bis(trimethylsilyl)thymine is a synthetic nucleoside that is used in the synthesis of DNA and RNA. It is a chloride-free nucleoside that contains an organic solvent, which makes it suitable for use in vitro tests. O,O'-Bis(trimethylsilyl)thymine has been shown to cause immunodeficient mice to produce antibodies when injected with this drug. It also has conformational properties that are similar to natural thymine, making it useful for nucleotide syntheses. O,O'-Bis(trimethylsilyl)thymine can be desulfurized by the enzyme desulfoviridin, which can increase its uptake by cells.

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Cy5.5 diacid, SE is commonly used in biomolecular labeling, fluorescence imaging and other fluorescence biological analysis.

6-Methoxy-9H-purine is an analog of adenosine and has been shown to have anticancer activity in vivo. It inhibits the growth of virus by binding to the viral DNA polymerase, thereby inhibiting viral replication. 6-Methoxy-9H-purine has also been shown to be active against cancer cells that are resistant to other anticancer agents, such as herpes simplex virus. The drug is currently undergoing toxicity studies in rats and dogs. 6-Methoxy-9H-purine can be administered orally or by intravitreal injection. Intravitreal injection is a method where the drug is injected into the eye through a needle. This route of administration may reduce systemic toxicity because it leaves less drug in the bloodstream.

Applications A metabolite of the potent and selective inhibitor of HIV-1 replication, AZT. References Brehm, J., et al.: Biochem., 47, 14020 (2008), von Kleist, M., et al.: Eur. J. Pharm. Sci., 36, 532 (2009),

Applications Reagent used in the preparation of Antithyroid agents. References Toropov, A., et al.: Eur. J. Med. Chem., 45, 3581 (2010), Daniels, C., et al>.: J. Bacteriol., 192, 2169 (2010), Castillo-Garit, J., et al.: Eur. J. Pharm. Sci., 39, 30 (2010),

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Eritadenine is a glycoside that has been found in the edible roots of plants belonging to the family Euphorbiaceae. Eritadenine is an inhibitor of malonic acid, which is a precursor for fatty acid synthesis. It has also been shown to have biological properties, such as inhibiting fat cell growth and reducing cholesterol levels in rats. Eritadenine can be detected with an analytical method that uses high-performance liquid chromatography coupled with a photodiode array detector. This method separates and identifies eritadenine from other compounds using polymerase chain reaction amplification on camp levels and sodium salts. Eritadenine can also be found in samples of liver cells or ethanolamine.

Applications 6-Amino-5-1,3-dimethyl-5-(formamido)uracil is a substitued uracilic metabolite of methylxanthine and is also a metabolite of Theophylline (T343850). 6-Amino-5-1,3-dimethyl-5-(formamido)uracil has been used for the synthesis of 8-arylaminotheophyllines. References Peri, G., et. al.: Toxicol. Lett., 18, 133 (1983); Celardo, A., et. al.: Eur. J. Drug Metab. Ph., 10, 279 (1985); Senga, K., et. al.: J. Heterocyclic Chem., 15, 641 (1978)

2’-Chloro-2’-deoxy-5-methyluridine is a prodrug that is converted to 5-fluoro-2'-deoxyuridine monophosphate (5FdUMP) in mammalian cells. This conversion is catalyzed by cytidine deaminase, which converts the 2' position of the sugar moiety to an amino group. In mammalian cells, this conversion occurs at a low rate and requires incubation. The 5FdUMP derivative is then phosphorylated by deoxycytidine kinase to form 5-fluorouracil, which inhibits DNA synthesis and replication. The cytosine residues in DNA are converted to uracil residues, resulting in misreading of the genetic code. This leads to cell death due to depletion of cellular energy stores and eventual DNA fragmentation. Radiation enhances the effect of 2'chloro-2'-deoxy-5-methyluridine as it increases cytosine

6-Amino-1,3-dipropyl-5-nitrosouracil is a xanthine derivative that exhibits selectivity for adenosine A1 receptors. It binds to the receptor with high affinity and blocks the binding of adenosine. The compound also has an affinity for other adenosine receptors, including A2 and A3. 6-Amino-1,3-dipropyl-5-nitrosouracil has been shown to block the respiratory depressant effects of caffeine and theophylline in rats and dogs. This drug may be useful in treating bronchial asthma or chronic obstructive pulmonary disease (COPD).

Applications Protected guanine References Tretyakova, N., et al.: Chem. Res. Toxicol., 20, 284 (2007), Rana, S., et al.: Bioorg. Med. Chem. Lett., 19, 670 (2009),

5-Pyrrolidinomethyluridine is a nucleic acid which is an analog of uridine. It can be used to inhibit the synthesis of RNA and DNA by binding reversibly to ribonucleotide reductase and deoxyribonucleotide reductase, respectively. 5-Pyrrolidinomethyluridine also inhibits the production of mitochondrial respiratory chain complex I, which reduces oxidative phosphorylation by inhibiting ATP production. This drug has been shown to have anti-inflammatory activities in mice due to its ability to inhibit prostaglandin synthesis.

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