B-hydroxy-1,2-oxaborolanes (benzoxaboroles) are extremely valuable synthetic and pharmaceutical intermediates.  We have been working on the development of novel synthetic methodologies for the synthesis of functionalized benzoxaboroles as potential therapeutic agents.  Previously, we have synthesized several benzoxaboroles employing Baylis-Hillman, Barbier allylation, and Passerini reaction protocols. In continuation of our interest on the development of structurally diverse benzoboroxoles, we synthesized several novel derivatives starting from 2-formylphenylboronic acid utilizing aldol reaction as the key step. All the synthsized benzoxaboroles have been evaluated for their anti-bacterial (gram postive, and gram negative), anti-fungal (candida), and anti-cancer (breast MCF-7, and multiple myeloma RPMI-8226) activities.  Our synthetic and biological evaluation studies will be presented in this paper.

Synthesis and biological evaluation of novel benzoxaboroles as potential antimicrobial and anticancer agents

243rd National Meeting (2012)

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