56045-73-9Relevant articles and documents
Norepinephrine-Transporter-Targeted and DNA-Co-Targeted Theranostic Guanidines
Kortylewicz, Zbigniew P.,Coulter, Donald W.,Han, Guang,Baranowska-Kortylewicz, Janina
supporting information, p. 2051 - 2073 (2020/03/31)
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.
Synthesis of Analogues of 5-Iodo-2'-deoxyuridine-5'-diphosphate
Jennings, L. John,Macchia, Marco,Parkin, Ann
, p. 2197 - 2202 (2007/10/02)
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
Anti herpes simplex viral compounds and their synthesis
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, (2008/06/13)
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.