Synthesis of conjugates of L-fucose and ortho-carborane as potential agents for boron neutron capture therapy

2002 ◽  
Vol 80 (8) ◽  
pp. 943-948 ◽  
Author(s):  
Prakriti Basak ◽  
Todd L Lowary

The synthesis of three potential boron neutron capture therapy agents (6–8) is reported. The compounds synthesized are comprised of ortho-carborane covalently attached to L-fucose via C-6. Incorporation of the carborane moiety was achieved either through the reaction of an L-fucose-derived alkyne with decaborane or by the coupling of a 6-amino-L-galactopyranose derivative with carborane carboxylic acid chloride (18).Key words: L-fucose, fucosyltransferase, boron neutron capture therapy, ortho-carborane.

2019 ◽  
Vol 48 (29) ◽  
pp. 10834-10844 ◽  
Author(s):  
Martin Kellert ◽  
Dennis J. Worm ◽  
Paul Hoppenz ◽  
Menyhárt B. Sárosi ◽  
Peter Lönnecke ◽  
...  

Boron-rich carboxylic acid derivatives were synthesised as coupling partners for tumour-selective biomolecules with applications as selective BNCT agents.


2020 ◽  
Vol 49 (1) ◽  
pp. 57-69 ◽  
Author(s):  
Martin Kellert ◽  
Paul Hoppenz ◽  
Peter Lönnecke ◽  
Dennis J. Worm ◽  
Bernd Riedl ◽  
...  

Introduction of a galactopyranosyl moiety in s-triazine-based boron-rich carboxylic acids and amines results in soluble and suitable coupling partners for tumour-selective biomolecules with applications in boron neutron capture therapy (BNCT).


Molecules ◽  
2019 ◽  
Vol 24 (18) ◽  
pp. 3288 ◽  
Author(s):  
Martin Kellert ◽  
Peter Lönnecke ◽  
Bernd Riedl ◽  
Johannes Koebberling ◽  
Evamarie Hey-Hawkins

The amount of boron accumulated in tumor tissue plays an important role regarding the success of the boron neutron capture therapy (BNCT). In this article, we report a modular system, combining readily available starting materials, like glycine, 1,3,5-triazine and the well-known 9-mercapto-1,7-dicarba-closo-dodecaborane(12), as well as α-d-galactopyranose for increased hydrophilicity, with a novel boron-rich tris-meta-carboranyl thiol.


2020 ◽  
Vol 22 (Supplement_3) ◽  
pp. iii345-iii345
Author(s):  
Hsin-Hung Chen ◽  
Yi-Wei Chen

Abstract A 6 y/o girl with recurrent multifocal glioblastoma received 3 times of boron neutron capture therapy (BNCT) and chimeric antigen receptor (CAR)–engineered T cells targeting the tumor-associated antigen HER2. Multiple infusions of CAR T cells were administered over 30 days through intraventricular delivery routes. It was not associated with any toxic effects of grade 3 or higher. After BNCT and CAR T-cell treatment, regression of all existing intracranial lesions were observed, along with corresponding increases in levels of cytokines and immune cells in the cerebrospinal fluid, but new lesions recurred soon after the treatment. This clinical response continued for 14 months after the initiation of first recurrence.


2021 ◽  
Author(s):  
Jing He ◽  
Heng Yan ◽  
Yanrong Du ◽  
Yan Ji ◽  
Fei Cai ◽  
...  

A reliable copper-mediated nucleophilic radiosynthesis of the BNCT-oriented PET probe [18F]FBPA was developed using novel aryldiboron precursors.


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