Professor and Department Head, Robert Vince Endowed Chair, McKnight Presidential Chair in Medicinal Chemistry, Department of Medicinal Chemistry, College of Pharmacy
Director, Institute for Therapeutics Discovery and Development, College of Pharmacy

georg239@umn.edu
612-626-6320 — office
Preferred method of contact: e-mail

Dr. Georg is professor and department head for the College of Pharmacy's Department of Medicinal Chemistry, where she holds the Robert Vince Endowed Chair and McKnight Presidential Chair. She is director of the Institute for Therapeutics Discovery and Development.

Before coming to the University of Minnesota in 2007, Dr. Georg was a University Distinguished Professor at the University of Kansas in Lawrence. At the University of Kansas she was also director of the Center for Drug Discovery at the Higuchi Biosciences Center and director of the Experimental Therapeutics Program for the Kansas Masonic Cancer Research Institute. She received her Ph.D. in 1980 and completed a post-doctoral fellowship in 1981 at Philipps Universität Marburg, Institut für Pharmazeutische Chemie, Germany; and she completed a post-doctoral fellowship in 1983 at the University of Ottawa, Canada. She was an assistant professor of medicinal chemistry for the School of Pharmacy, University of Rhode Island, Kingston in 1983-84 before joining the faculty at the University of Kansas in 1984.

Research Interests

Medicinal chemistry, drug discovery, high throughput screening, combinatorial chemistry, chemical biology, organic chemistry, natural products chemistry, cancer, Alzheimer's disease, male contraception.

Selected Publications

Hutt, O. E., Reddy, B. S.; Nair, S. K.; Reiff, E. A.; Henri, J. T.; Greiner, J. F.; Chiu, T.-L., VanderVelde, D. G.; Amin, E. A.; Himes, R. H.; Georg, G.I. Total Synthesis and Evaluation of C25-Benzyloxyepothilone C for Tubulin Assembly and Cytotoxicity Against MCF-7 Breast Cancer Cells. Bioorg. Med. Chem. Lett. 2008, 18, 4904-4906.

Santhapuram, H. K. R.; Datta, A.; Hutt, O.; Georg, G. I. N-Methylation of the C-3' Amide of Taxanes: Synthesis of N-Methyltaxol and N-Methylpaclitaxel. J. Org. Chem. 2008, 73, 4705-4708.

Kimball, S. F.; Himes, R. H.; Georg, G. I. Synthesis and Evaluation of Heteroaromatic 6,7-diary-2,3,8,8a-tetrahydroindolizin-5(1H)-ones for Cytotoxicity a Against the HCT-116 Colon Cancer Cell Line. Bioorg. Med. Chem. Lett. 2008, 18, 3248-3250.

Kimball. S. F.; Turunen, B. J.; Ellis, K.; Georg, G. I.; 8 Himes, R. H. Enantiospecific Synthesis and Cytotoxicity of 7-(4-Methoxyphenyl)-6-phenyl-2,3,8,8a-tetrahydroindolizin-5(1H)-one Enantiomers. Bioorg. Med. Chem. 2008, 16, 4367-4377.

Dutta, D.; Datta, A.; Vander Velde, D. G.; Georg, G. I. Oxidation of Baccatin III at C14: A Facile Rearrangement of the Baccatin III Core. Lett. Org. Chem. 2007, 4, 151-145.

Kimball, F. S.; Tunoori, A. R.; Victory, S.; Dutta D.; White, J.; Himes, R. H.; Georg, G. I. Synthesis, in vitro, and in vivo Cytotoxicity of 6,7-Diaryl-2,3,8,8a-tetrahydroindolizin-5(1H)-ones. Bioorg. Med. Chem. Lett. 2007, 17, 4703-4707.

Ahn, Y.; Vogeti, L.; Liu, C.-J.; Santhapuram, H. K. R.; White, J M.; Mitscher, L. A.; Lushington, G. H.; Hanson, P. R.; Powell, D.; R. Himes, R. H.; Huff, J. K.; Roby, K. F.; Georg, G. I. Design, Synthesis, Antiproliferative and CDK2-Cyclin A Inhibitory Activity of Novel Flavopiridol Analogues. Bioorg. Med. Chem. 2007, 15, 702-713.

Ge, H.; Spletstoser, J. T.; Yang, Y.; Kayser, M; Georg, G. I. Synthesis of Docetaxel and Butitaxel Analogues Through Kinetic Resolution of Racemic beta-Lactams With 7-O-Triethylsilylbaccatin III. J. Org. Chem. 2007, 72, 756-759.

Blackman, B.; Georg, G. I.; Lushington, G. H. CoMSIA/QSAR Models for Vacuolar (H+) ATPase Inhibition by Selected Benzoates and Benzolactone Species. Letters Drug Des. 2006, 3, 104-107.

Ge, H.; Himes, R. H.; Vasandani, V.; Audus, K. L.; Seelig, A.; Huff, J.; Georg, G. I. Synthesis and Interactions of 7-Deoxy, 10-Deoxy and 7,10-Dideoxypaclitaxel with NCI/ADR-RES Cancer Cells and Bovine Brain Microvessel Endothelial Cells. Bioorg. Med. Chem. Lett. 2005, 16, 433-436.

Spletstoser, J. T.; Turunen, B. J.; Desino, K.; Rice, A.; Dutta, A.; Datta, D.; Huff, J. K.; Himes, R. H.; Audus, K. L.; Seelig, A.; Georg, G. I. Single-site Chemical Modification at C10 of the Baccatin Core of Paclitaxel Analogs Reduces P-Glycoprotein Interactions in Bovine Brain Microvessel Endothelial Cells and Retains Cytotoxicity. Bioorg. Med. Chem. Lett. 2006, 16, 495-498.

Haack, T.; Haack, K.; Diederich, W.; Blackman, B.; Georg, G. I. Formal Total Synthesis of (-)-Salicylihalamides A and B from D-Glucose and L-Rhamnose. J. Org. Chem. 2005, 70, 7592-7604.

Barboni, L.; Giarlo, G.; Ricciutelli, M,;  Ballini, R.; Georg, G. I.; Vander Velde, D. G.; Himes, R. H.; Wang, M.; Lakdawala, S.; Snyder, J. P. Synthesis, Modeling and anti-Tubulin Activity of a D-Desco Paclitaxel Analog. Org. Lett. 2004, 6, 461-464.

Rice, A.; Liu, Y.; Michaelis, M.-L.; Himes, R. H., Georg, G. I.; Audus, K. L. Chemical Modification of Paclitaxel (Taxol) Reduces P-Glycoprotein Interactions and Increases Permeation Across the Blood-Brain Barrier in vitro and in situ. J. Med. Chem. 2005, 48, 832-838.

Buck, S. B.; Huff, J. K.; Himes, R. H.; Georg, G. I. Total Synthesis and Anti-Tubulin Activity of Epi-C3 Analogues of Cryptophycin-24. J. Med. Chem. 2004, 47, 3697-3699.

Spletstoser, J. T.; Flaherty, P. T.; Himes, R. H.; Georg, G. I. Synthesis and Biological Evaluation of a 3'-(4-Azidophenyl)-3-dephenylpaclitaxel Photoaffinity Probe. J. Med. Chem. 2004, 47, 6459-6465.

Buck, S. B.; Huff, J. K.; Himes, R. H.; Georg, G. I. Total Synthesis and Anti-tubulin Activity of C10 Analogues of Cryptophycin-24. J. Med. Chem. 2004, 47, 696-702.

Rice, A.; Michaelis, M. L.; Georg, G.; Liu, Y.; Turunen, B.; Audus. K. L. Overcoming the Blood-Brain Barrier to Taxane Delivery for Neurodegenerative Diseases and Brain Tumors. J. Mol. Neurosci. 2003, 20, 339-343

Gupta, M. L.; Bode, C.; Georg, G. I.; Himes, R. H. Understanding Tubulin-Taxol Interactions That Impart Taxol Binding to Yeast Tubulin. Proc. Natl. Acad. Sci. U.S.A. 2003, 100, 6394-6397.