Anti-Cancer Agents in Medicinal Chemistry

(Formerly Current Medicinal Chemistry - Anti-Cancer Agents)

Michelle Prudhomme  
Universite Blaise Pascal - C.N.R.S
Aubiere Cedex


3-Carboranyl Thymidine Analogues (3CTAs) and Other Boronated Nucleosides for Boron Neutron Capture Therapy

Author(s): Youngjoo Byun, Sureshbabu Narayanasamy, Jayaseharan Johnsamuel, Achintya K. Bandyopadhyaya, Rohit Tiwari, Ashraf S. Al-Madhoun, Rolf F. Barth, Staffan Eriksson and Werner Tjarks

Affiliation: College of Pharmacy, TheOhio State University, Columbus, OH, USA.


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.

Keywords: Boron neutron capture therapy, carboranes, nucleosides, thymidine kinase, 3-carboranyl thymidine analogues, 3CTAs, N5-2OH

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Article Details

Page: [127 - 144]
Pages: 18
DOI: 10.2174/187152006776119171
Price: $58