Small-molecule anticancer agents containing boron have attracted growing attention due to their unique chemical properties and promising anticancer activities. This review systematically summarizes recent advances in developing boron-based small-molecule agents, highlighting their molecular structures, mechanisms of action, and therapeutic applications. Specifically, it covers key categories such as boron neutron capture therapy (BNCT) agents, boron-based enzyme inhibitors, novel benzoxaborole derivatives, and boron-based reactive oxygen species (ROS)-targeting agents. The challenges associated with these boron-containing drugs, including limited tumor selectivity, suboptimal boron accumulation, and low bioavailability, are also highlighted. Additionally, it offers perspectives on future directions in the field, providing insights intended to guide ongoing research and development in boron-based anticancer therapies.
Guo et al. (Wed,) studied this question.