TY - JOUR
T1 - 3-carboranyl thymidine analogues (3CTAs) and other boronated nucleosides for boron neutron capture therapy
AU - Byun, Youngjoo
AU - Narayanasamy, Sureshbabu
AU - Johnsamuel, Jayaseharan
AU - Bandyopadhyaya, Achintya K.
AU - Tiwari, Rohit
AU - Al-Madhoun, Ashraf S.
AU - Barth, Rolf F.
AU - Eriksson, Staffan
AU - Tjarks, Werner
PY - 2006/3
Y1 - 2006/3
N2 - 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.
AB - 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.
KW - 3-carboranyl thymidine analogues
KW - 3CTAs
KW - Boron neutron capture therapy
KW - Carboranes
KW - N5-2OH
KW - Nucleosides
KW - Thymidine kinase
UR - http://www.scopus.com/inward/record.url?scp=33645826248&partnerID=8YFLogxK
UR - http://www.scopus.com/inward/citedby.url?scp=33645826248&partnerID=8YFLogxK
U2 - 10.2174/187152006776119171
DO - 10.2174/187152006776119171
M3 - Article
C2 - 16529536
AN - SCOPUS:33645826248
SN - 1871-5206
VL - 6
SP - 127
EP - 144
JO - Anti-Cancer Agents in Medicinal Chemistry
JF - Anti-Cancer Agents in Medicinal Chemistry
IS - 2
ER -