The regulation of foreign gene expression can be problematic due to issues including non-specific effects on other (non-target) genes, leakiness, instability, toxicity, and/or undesirable side effects to the host. Improved ecdysone receptor-based gene regulation systems (e.g. those using diacylhydrazine (DAH) compounds) having superior physiochemical and/or pharmacological properties are desirable. The present disclosure provides boron-containing diacylhydrazines of Formula I and pharmaceutically acceptable salts and solvates thereof, wherein R1, R2, R3, R4, and R5 are defined as set forth in the specification. The compounds of the present invention can be beneficial in the precise control of gene expression by way of interacting with gene switches comprising a suitable binding domain for the compounds. The compounds can be used in pharmaceutical compositions and are advantageous in the treatment of diseases (e.g. various forms of cancer) due to their capacity to regulate gene expression via gene switches.
