We describe herein for the first time our medicinal electronomics bricolage design of
hypoxia-targeting
antineoplastic drugs and
boron tracedrugs as newly emerging
drug classes. A new area of
antineoplastic drugs and treatments has recently focused on neoplastic cells of the
tumor environment/microenvironment involving accessory cells. This
tumor hypoxic environment is now considered as a major factor that influences not only the response to
antineoplastic therapies but also the potential for malignant progression and
metastasis. We review our medicinal electronomics bricolage design of
hypoxia-targeting drugs, antiangiogenic hypoxic cell radiosensitizers,
sugar-hybrid hypoxic cell radiosensitizers, and
hypoxia-targeting 10B delivery agents, in which we design
drug candidates based on their electronic structures obtained by molecular orbital calculations, not based solely on pharmacophore development. These drugs include an antiangiogenic hypoxic cell radiosensitizer TX-2036, a
sugar-hybrid hypoxic cell radiosensitizer TX-2244, new
hypoxia-targeting
indoleamine 2,3-dioxygenase (IDO) inhibitors, and a
hypoxia-targeting BNCT agent, BSH (sodium borocaptate-10B)-hypoxic
cytotoxin tirapazamine (TPZ) hybrid
drug TX-2100. We then discuss the concept of
boron tracedrugs as a new
drug class having broad potential in many areas.