Boron in My Mind: A Comprehensive Review of the Evolution of the Diverse Syntheses of 4-Borono-l-Phenylalanine, the Leading Agent for Boron Neutron Capture Therapy.

IF 3.6 4区 医学 Q2 CHEMISTRY, MEDICINAL ChemMedChem Pub Date : 2025-03-12 DOI:10.1002/cmdc.202500059
Sarfraz Ahmad, Ming Pan, John Hayward, Massimo Sementilli, Lisa Porter, John F Trant
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Abstract

Boron Neutron Capture Therapy (BNCT) leverages the nuclear reaction between boron-10 and thermal neutrons to selectively destroy cancer cells while minimizing damage to surrounding healthy tissues. This therapy has found use in treating glioblastoma, which as a brain cancer, is difficult to treat using conventional radiotherapy, surgery, and chemotherapy due to location and the risk of brain damage. However, to work, the cells must contain 10B. 4-Borono-l-phenylalanine (l-BPA) is the most frequently used boron delivery agent in this therapy. Surprisingly, despite its seemingly simple structure, there is no consensus approach to making it-the synthesis of l-BPA has been approached through multiple routes, reflecting the challenges in producing high-purity, isotopically enriched material. When a new site is looking to make this essential material, it can be challenging to determine the best route for the situation as there is no critical analysis comparing and discussing the relative merits of the approaches. Herein, we comprehensively and critically examine and compare the reported methods, from both the academic and patent literature, used to synthesize l-BPA. The review also highlights the limitations of each method regarding scalability, cost-effectiveness, and safety, especially considering the high cost of isotopically enriched 10B.

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来源期刊
ChemMedChem
ChemMedChem 医学-药学
CiteScore
6.70
自引率
2.90%
发文量
280
审稿时长
1 months
期刊介绍: Quality research. Outstanding publications. With an impact factor of 3.124 (2019), ChemMedChem is a top journal for research at the interface of chemistry, biology and medicine. It is published on behalf of Chemistry Europe, an association of 16 European chemical societies. ChemMedChem publishes primary as well as critical secondary and tertiary information from authors across and for the world. Its mission is to integrate the wide and flourishing field of medicinal and pharmaceutical sciences, ranging from drug design and discovery to drug development and delivery, from molecular modeling to combinatorial chemistry, from target validation to lead generation and ADMET studies. ChemMedChem typically covers topics on small molecules, therapeutic macromolecules, peptides, peptidomimetics, and aptamers, protein-drug conjugates, nucleic acid therapies, and beginning 2017, nanomedicine, particularly 1) targeted nanodelivery, 2) theranostic nanoparticles, and 3) nanodrugs. Contents ChemMedChem publishes an attractive mixture of: Full Papers and Communications Reviews and Minireviews Patent Reviews Highlights and Concepts Book and Multimedia Reviews.
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