Dr David France
Our expertise lies in the de novo construction of molecules that have important biological functions. Two examples include sieboldine A, which has exhibited low micromolar inhibitory activity toward acetylcholinesterase (IC50 2.0 µM, similar to a compound that is currently undergoing clinical evaluation for the treatment of Alzheimer’s disease and schizophrenia), and chloptosin, a molecule that is reported to exhibit apoptotic activity in the apoptosis-resistant human pancreatic adenocarcinoma cell line AsPC-1 (with an EC50 of 1.6μm after 24h) as well as in several apoptosis-sensitive cancer cell lines.
Canham, S. M.; France, D. J.; Overman, L. E. “Total Synthesis of (+)-Sieboldine A” J. Am. Chem. Soc. 2010, 132, 7876–7877.
Oelke, A. J.; France, D. J.; Hofmann, T.; Wuitschik, G.; Ley, S. V. “Total Synthesis of Chloptosin” Angew. Chem., Int. Ed. 2010, 49, 6139–6142.