Boron has become a crucial weapon in anticancer research due to its significant intervention in cell proliferation. Being an excellent bio-isosteric replacement of carbon, it has modulated the anticancer efficacy of various molecules in the development pipeline. It has elicited promising results through interactions with various therapeutic targets such as HIF-1α, steroid sulfatase, arginase, proteasome, etc. Since boron liberates alpha particles, it has a wide-scale application in Boron Neutron Capture therapy (BNCT), a radiotherapy that demonstrates selectivity towards cancer cells due to high boron uptake capacity. Significant advances in the medicinal chemistry of boronated compounds, such as boronated sugars, natural/unnatural amino acids, boronated DNA binders, etc., have been reported over the past few years as BNCT agents. In addition, boronated nanoparticles have assisted the field of bio-nano medicines by their usage in radiotherapy. This review exclusively focuses on the medicinal chemistry aspects, radiotherapeutic, and chemotherapeutic aspects of boron in cancer therapeutics. Emphasis is also given on the mechanism of action along with advantages over conventional therapies.

由于硼对细胞增殖的显着干预作用，它已成为抗癌研究的重要武器。作为碳的优异生物电子等排替代品，它在开发过程中调节了各种分子的抗癌功效。它通过与各种治疗靶点（如 HIF-1α、类固醇硫酸酯酶、精氨酸酶、蛋白酶体等）相互作用，获得了有希望的结果。由于硼释放 α 粒子，因此在硼中子捕获疗法（BNCT）（一种放射疗法）中得到了广泛的应用这表明由于硼吸收能力高，对癌细胞具有选择性。过去几年，硼化合物（例如硼糖、天然/非天然氨基酸、硼化DNA结合剂等）作为BNCT剂在药物化学方面取得了重大进展。此外，硼化纳米颗粒通过在放射治疗中的应用，为生物纳米药物领域提供了帮助。本综述专门关注癌症治疗中硼的药物化学方面、放射治疗和化疗方面。还强调了作用机制以及相对于传统疗法的优势。