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 S. Al-Madhoun, Rolf F. Barth, Staffan Eriksson, Werner Tjarks

Research output: Contribution to journalArticlepeer-review

29 Scopus citations


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 (US)
Pages (from-to)127-144
Number of pages18
JournalAnti-Cancer Agents in Medicinal Chemistry
Issue number2
StatePublished - Mar 2006
Externally publishedYes


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

ASJC Scopus subject areas

  • Cancer Research
  • Molecular Medicine
  • Pharmacology


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