The natural compound Combretastatin A-4 and its derivatives; have been the leading scaffolds for the development of cancer pharmacophore designs. It has been a task throughout the research field to determine the backbones with biological potential. The chalcone-based products have been favored as candidates for therapeutic processes of cancer but also the treatment of bacteria and malaria. It has been reinforced in the literature that merging ferrocene in product designs enhances the potential of bioactive compounds. Furthermore, incorporating heterocycles as a modification to the compound structure, have been leading researchers for the strategy and potential enhancement of bioactive compounds. Among these types of moieties, the isoxazoles and epoxides had demonstrated potential as analgesic, anti-inflammatory, and anticancer forthcoming. Our synthetic approach envisions fully encompasses these features, stipulating an underlining to ferrocenyl chalcones and the incorporation of heterocycles to their structure. To procure our specific purpose, ferrocenyl chalcones have been synthesized via Claisen–Schmidt condensation in moderate to good yields. Moreover, precursors for epoxide derivatives have been achieved in moderate to good yields aiming for a Darzen reaction for the synthesis of epoxide products. Furthermore, isoxazole derivatives have been synthesized in moderate yields from ferrocenyl chalcones. Compounds have been characterized by 1H and 13C NMR spectra, cyclic voltammetry, and UV/VIS spectra. Synthetic methodology, characterization, and preliminary bioassays in cancer cell lines, bacteria, and malaria of these compounds will be elaborated. Research supported by RISE Grant number: 5R25GM061151-14

Towards the biological enhancement of ferrocenyl derivatives: An improvement with heterocyclic moieties

251st National Meeting (2016)

The official archive and repository for all ACS Meetings & Expositions abstracts and select posters or presentations.