Design, Synthesis, and Structure–Activity Relationship of 7‑Propanamide Benzoxaboroles as Potent Anticancer Agents

Benzoxaboroles, as a novel class
of bioactive molecules with unique
physicochemical properties, have been shown to possess excellent antimicrobial
activities with tavaborole approved in 2014 as an antifungal drug.
Although urgently needed, the investigation of benzoxaboroles as anticancer
agents has been lacking so far. In this study, we report the design,
synthesis, and anticancer structure–activity relationship of
a series of 7-propanamide benzoxaboroles. Compounds 103 and 115 showed potent activity against ovarian cancer
cells with IC50 values of 33 and 21 nM, respectively. Apoptosis
was induced by these compounds and colony formation was effectively
inhibited. Furthermore, they also showed excellent efficacy in ovarian
tumor xenograft mouse model.