3-carboranyl thymidine analogues (3CTAs) and other boronated nucleosides for boron neutron capture therapy

Youngjoo Byun, Sureshbabu Narayanasamy, Jayaseharan Johnsamuel, Achintya K. Bandyopadhyaya, Rohit Tiwari, Ashraf Al Madhoun, Rolf F. Barth, Staffan Eriksson, Werner Tjarks

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30 Citations (Scopus)

Abstract

One category of boron neutron capture therapy (BNCT) agents that has received extensive attention during recent years is 3-carboranyl thymidine analogues (3CTAs). These molecules are phosphorylated to the corresponding 5′-monophosphates by human thymidine kinase 1 (TK1), an enzyme that is up-regulated in dividing malignant cells. Thus, these phosphorylated molecules are selectively entrapped in tumor cells due to the acquired negative charge. This review will analyze design strategies applied for the synthesis of boron-containing nucleosides in general and in particular reference to 3CTAs. Results of biological studies with these molecules will be discussed.

Original languageEnglish
Pages (from-to)127-144
Number of pages18
JournalAnti-Cancer Agents in Medicinal Chemistry
Volume6
Issue number2
DOIs
Publication statusPublished - 1 Mar 2006

Keywords

  • 3-carboranyl thymidine analogues
  • 3CTAs
  • Boron neutron capture therapy
  • Carboranes
  • N5-2OH
  • Nucleosides
  • Thymidine kinase

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    Byun, Y., Narayanasamy, S., Johnsamuel, J., Bandyopadhyaya, A. K., Tiwari, R., Al Madhoun, A., Barth, R. F., Eriksson, S., & Tjarks, W. (2006). 3-carboranyl thymidine analogues (3CTAs) and other boronated nucleosides for boron neutron capture therapy. Anti-Cancer Agents in Medicinal Chemistry, 6(2), 127-144. https://doi.org/10.2174/187152006776119171