**4. Conclusion**

In this review, we summarize the current state of knowledge regarding the design and synthesis of 10B and/or 11B containing agents for biomedical applications such as 11B NMR probes and BNCT agents. We developed the d-block metal ion probes based on changes in 11B NMR signals due to the hydrolysis of C–B bond in **7** (L1 ) and **8** (L2 ) and the decomposition of *o*-carborane moieties in derivatives such as **14** and **16** (L5 ) upon complexation with metal ions in aqueous solution at physiological pH. Some novel BNCT agents based on sugar and macrocyclic polyamine scaffolds were also designed and synthesized. The findings indicate that 10B-enriched monomeric macrocyclic polyamines **10B-48b** (L9 ) and **10B-49a** (L10) exhibit potent BNCT activity upon thermal neutron irradiation, possibly due to interaction with DNA, resulting in the efficient damage of DNA molecules that are in close proximity to the boron compounds.

We believe that this review provides useful information for the future design and synthesis of novel boron-containing compounds and their applications for the treatment and diagnosis of cancer and other diseases, as well as in related research fields.
