title: 3-Carboranyl thymidine analogues (3CTAs) and other boronated nucleosides for boron neutron capture therapy.
abstract: 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.
authors.affiliation: College of Pharmacy, The Ohio State University, Columbus, OH, USA.
authors.forename: Youngjoo
authors.initials: Y
authors.lastname: Byun
authors.forename: Sureshbabu
authors.initials: S
authors.lastname: Narayanasamy
authors.forename: Jayaseharan
authors.initials: J
authors.lastname: Johnsamuel
authors.forename: Achintya K
authors.initials: AK
authors.lastname: Bandyopadhyaya
authors.forename: Rohit
authors.initials: R
authors.lastname: Tiwari
authors.forename: Ashraf S
authors.initials: AS
authors.lastname: Al-Madhoun
authors.forename: Rolf F
authors.initials: RF
authors.lastname: Barth
authors.forename: Staffan
authors.initials: S
authors.lastname: Eriksson
authors.forename: Werner
authors.initials: W
authors.lastname: Tjarks
mesh_terms: 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
chemical_list: D000970:Antineoplastic Agents; D001880:Boranes; D009705:Nucleosides; D009711:Nucleotides; D011741:Pyrimidine Nucleosides; D013937:Thymidine Kinase; C092717:thymidine kinase 1; D013936:Thymidine