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

ISSN: 1875-5992 (Online)
ISSN: 1871-5206 (Print)

Volume 16, 12 Issues, 2016

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Anti-Cancer Agents in Medicinal Chemistry

Formerly: Current Medicinal Chemistry - Anti-Cancer Agents

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

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

Anti-Cancer Agents in Medicinal Chemistry, 6(2): 127-144.

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.


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

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Article Details

Volume: 6
Issue Number: 2
First Page: 127
Last Page: 144
Page Count: 18
DOI: 10.2174/187152006776119171
Price: $58

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