3-Carboranyl thymidine analogues (3CTAs) and other boronated nucleosides for boron neutron capture therapy.
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.
Byun
Youngjoo
Y
College of Pharmacy, The Ohio State University, Columbus, OH, USA.
Narayanasamy
Sureshbabu
S
Johnsamuel
Jayaseharan
J
Bandyopadhyaya
Achintya K
AK
Tiwari
Rohit
R
Al-Madhoun
Ashraf S
AS
Barth
Rolf F
RF
Eriksson
Staffan
S
Tjarks
Werner
W
D000818:Animals; D000970:Antineoplastic Agents / Q000138:chemical synthesis / Q000627:therapeutic use; D001880:Boranes / Q000138:chemical synthesis* / Q000627:therapeutic use; D016754:Boron Neutron Capture Therapy / Q000379:methods*; D006801:Humans; D009705:Nucleosides / Q000138:chemical synthesis* / Q000627:therapeutic use; D009711:Nucleotides / Q000138:chemical synthesis / Q000627:therapeutic use; D011741:Pyrimidine Nucleosides / Q000138:chemical synthesis / Q000627:therapeutic use; D013936:Thymidine / Q000031:analogs & derivatives* / Q000138:chemical synthesis; D013937:Thymidine Kinase / Q000378:metabolism
D000970:Antineoplastic Agents; D001880:Boranes; D009705:Nucleosides; D009711:Nucleotides; D011741:Pyrimidine Nucleosides; D013937:Thymidine Kinase; C092717:thymidine kinase 1; D013936:Thymidine