56045-73-9

Upstream product

• 58349-30-7 5-Iodo-5'-azido-2',5'-dideoxyuridine 
• 54-42-2 5-Iodo-2'-deoxyuridine 
• 58349-27-2 2'-deoxy-5-iodo-5'-O-(p-toluenesulfonyl)uridine 
• 27999-47-9 ((2R,3S,5R)-5-(2,4-dioxo-3,4-dihydropyrimidin-1(2H)-yl)-3-hydroxytetrahydrofuran-2-yl)methyl 4-methylbenzenesulfonate 
• 35959-37-6 5’-azido-2’,5’-dideoxyuridine 
• 35959-38-7 5'-Amino-2',5'-dideoxy-uridine 

Downstream Products

• 119423-53-9 5'-[2-(2,6-dichlorophenyl)acetamido]-2',5'-dideoxy-5-iodouridine 

Relevant academic research and scientific papers

Norepinephrine-Transporter-Targeted and DNA-Co-Targeted Theranostic Guanidines

High risk neuroblastoma often recurs, even with aggressive treatments. Clinical evidence suggests that proliferative activities are predictive of poor outcomes. This report describes syntheses, characterization, and biological properties of theranostic guanidines that target norepinephrine transporter and undergo intracellular processing, and subsequently their catabolites are efficiently incorporated into DNA of proliferating neuroblastoma cells. Radioactive guanidines are synthesized from 5-radioiodo-2′-deoxyuridine, a molecular radiotherapy platform with clinically proven minimal toxicities and DNA-targeting properties. The transport of radioactive guanidines into neuroblastoma cells is active as indicated by the competitive suppression of cellular uptake by meta-iodobenzylguanidine. The rate of intracellular processing and DNA uptake is influenced by the agent's catabolic stability and cell population doubling times. The radiotoxicity is directly proportional to DNA uptake and duration of exposure. Biodistribution of 5-[125I]iodo-3′-O-(?-guanidinohexanoyl)-2′-deoxyuridine in a mouse neuroblastoma model shows significant tumor retention of radioactivity. Neuroblastoma xenografts regress in response to the clinically achievable doses of this agent.

MIBG ANALOGS AND USES THEREOF

Compounds and compositions for targeting cells expressing norepinephrine transporter, and methods of making and using the same. The compounds comprise MIBG analogs conjugated to active agents for treatment and/or diagnosis of various conditions, including neuroblastoma.

Synthesis of Analogues of 5-Iodo-2'-deoxyuridine-5'-diphosphate

The synthesis of three types of diphosphate analogues of 5-iodo-2'-deoxyuridine-5'-diphosphate is reported.Routes are described to the 5'-phosphonoacetamido, the 5'-N-phosphonosulfamoyl and the 5'-O-sulfamoylcarbamoyl derivatives, 2, 3 and 4 starting from

A novel synthesis and biological activity of several 5-halo-5'-amino analogues of deoxyribopyrimidine nucleosides.

A novel synthetic procedure has been developed for the large-scale synthesis of 5-chloro-, 5-bromo-, and 5-iodo-5'-amino-2',5'-dideoxyuridine (4c-e) as well as of two new analogues, 5-iodo-5'-amino-2',5'-dideoxycytidine and 5-fluoro-5'-amino-2',5'-dideoxyuridine (4a and 4b), in good yield. The starting materials, 5-halo-2'-deoxyuridine and 5-halo-2'-deoxycytidine, are readily available and the method is straightforward. This report describes the synthesis and the biologial activities of these compounds.

Anti herpes simplex viral compounds and their synthesis

The compounds 5'-amino-2',5'-dideoxy-5-iodouridine; 5'-amino-2',5'-dideoxy-5-bromouridine; and the pharmaceutically acceptable acid addition salts thereof have been found to be potent inhibitors of herpes simplex virus.