119644-23-4Relevant articles and documents
Radiolabeled cyclosaligenyl monophosphates of 5-iodo-2′-deoxyuridine, 5-iodo-3′-fluoro-2′,3′-dideoxyuridine, and 3′-fluorothymidine for molecular radiotherapy of cancer: Synthesis and biological evaluation
Kortylewicz, Zbigniew P.,Kimura, Yu,Inoue, Kotaro,MacK, Elizabeth,Baranowska-Kortylewicz, Janina
, p. 2649 - 2671 (2012/06/16)
Targeted molecular radiotherapy opens unprecedented opportunities to eradicate cancer cells with minimal irradiation of normal tissues. Described in this study are radioactive cyclosaligenyl monophosphates designed to deliver lethal doses of radiation to cancer cells. These compounds can be radiolabeled with SPECT- and PET-compatible radionuclides as well as radionuclides suitable for Auger electron therapies. This characteristic provides an avenue for the personalized and comprehensive treatment strategy that comprises diagnostic imaging to identify sites of disease, followed by the targeted molecular radiotherapy based on the imaging results. The developed radiosynthetic methods produce no-carrier-added products with high radiochemical yield and purity. The interaction of these compounds with their target, butyrylcholinesterase, depends on the stereochemistry around the P atom. IC50 values are in the nanomolar range. In vitro studies indicate that radiation doses delivered to the cell nucleus are sufficient to kill cells of several difficult to treat malignancies including glioblastoma and ovarian and colorectal cancers.
Synthesis and Antiviral Evaluation of Some 3′-Fluoro Bicyclic Nucleoside Analogues
McGuigan, Christopher,Carangio, Antonella,Snoeck, Robert,Andrei, Graciela,De Clercq, Erik,Balzarini, Jan
, p. 1 - 5 (2007/10/03)
The synthesis of 3′-fluoro analogues of recently discovered highly potent anti-VZV furanopyrimidine deoxynucleosides (BCNAs) is herein reported, for both the alkyl and alkylphenyl series. The compounds are tested against a range of herpes viruses and disp
Antiviral compounds
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, (2008/06/13)
2',3'-Dideoxy-3'-fluoro pyrimidine nucleosides particularly 2',3'-dideoxy-3'-fluorothymidine have been found to have particularly potent activity against adenovirus infections especially those caused by adenoviruses of serotype 8. Such compounds are preferably presented in pharmaceutical formulations adapted for ophthalmic administration.
