Division of Science, Mathematics, and Computing presents
Silicon Drug Design as a Driver of X-ray Structural Characterization in the Undergraduate Classroom
Friday, March 8, 2013
A lecture by
Candidate for the visiting position in Chemistry
Various cancer cell types display elevated expression of cyclooxygenase-2 (COX-2) expression. Patients with elevated COX-2 that receive a COX-2 inhibitor have demonstrated improved survival. Indomethacin (IM) is a COX-non-selective inhibitor with demonstrated anticancer activity in patients. The anticancer effects of IM are related to inhibition of COX-2 as well as COX-independent targets. Herein the synthesis and activity of novel IM-sila- amide derivatives where strategic silicon addition results in COX-2 selective IM derivatives that are devoid of the COX-1 associated toxicities is discussed.
Moreover, both pharmaceutical and chemical modifications aimed at improved solubility will be reviewed. A synthetic methodology incorporating a heteroatom in the amino-functional silane has been developed and used to generate second-generation sila-IM derivatives that could have improved pharmacological properties. The polyether linkages can in the silane side chain can be expanded to accommodate varying degrees of hydrophilicity. Lastly, the use of key synthetic intermediates in evaluating the Bruker SMART X2S bench-top system as a means to making X-ray crystallography more mainstream in the undergraduate classroom will be related.
Location: RKC 115
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