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Wednesday, April 26 • 8:30am - 10:00am
Synthesis of Anticancer ad DNA Cleaving compounds from Combretastatin A-4

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Combretastatin A-4, a naturally occurring compound, isolated from the South African bush willow Combretum Caffrum, has analogs which have demonstrated to provide antibacterial, anti mitotic, anticancer, and antibiotic properties. This research consists of two foci, one for each project: (1) to increase the solubility and biological activity of analogs of Combretastatin A-4 in order to stop cancerous cells from replicating and (2) to induce DNA cleavage via the electrocyclization of derivatives of these analogs. Derivatives of the chalcone backbone will be the basis for the first focus, specifically, Lamellarin pyrroles. These pyrroles have proven to be positively bioactive in the apoptosis of cancerous and multidrug resistant (MDR) cells. Analogs of Lamellarins are recognized to have strong biological potency due to the five-membered nitrogenous ring and the relationship of the planarity between its ABCDE rings. For the first project, derivatives of the Lamellarins pyrrole analogs will serve the purpose of prohibiting cell division by acting as a substrate to bind to the beta-tubulin colchicine binding site during the metaphase stage of mitosis. The binding will occur via the trimethoxy feature of the A ring as the key. Furthermore, modifying the functional groups on the B rings can increase the solubility and biological activity within the bloodstream. For the second project, ynediene electrocyclizations of the Lamellarin pyrroles produce heterocyclic di-radicals which may have the ability to act as an unstable warhead to potentially induce DNA cleavage.

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Wednesday April 26, 2017 8:30am - 10:00am
Concourse - Wilma Sherrill Center