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William Roush, Ph.D.

Professor
Associate Dean of Graduate Studies
Department of Chemistry
Florida Campus
Laboratory Website
roush@scripps.edu
(561) 228-2450

Scripps Research Joint Appointments

Executive Director, Medicinal Chemistry
Faculty, Graduate Program

Research Focus

The major focus of our research effort concerns the synthesis of stereochemically complex, biologically active natural products. Natural products of considerable current interest include (among others): durhamycin A and B, members of the aureolic acid antibiotic family; angelimicin B, a signal transduction pathway inhibitor; tedanolide, scytophycin C, apoptolidin, and superstolide A -- four structurally complex macrolide antibiotics; quartromicin D, an antiviral agent; and various members of the amphidinolide and Annonaceous acetogenin families. Significant emphasis is placed on the discovery, development, and/or illustration of new reactions and synthetic methods in this research. Some of these synthesis projects involve intramolecular cycloaddition reactions. Others make use of acyclic diastereoselective or enantioselective stereochemical techniques. Still others focus on the development and illustration of new methods for synthesis of glycosides.

We are also pursuing several research programs in bioorganic chemistry, chemical biology and medicnal chemistry, including one focusing on the design and synthesis of inhibitors of cysteine proteases isolated from tropical parasites. This project is performed in collaboration with several groups of scientists at the University of California, San Francisco and the Unversity of California, San Diego. Additional projects in my laboratory at Scripps Florida include efforts to develop potent, selective inhibitors of several kinases and proteases, inhibitors of certain epigenetic targets, inhibitors (inverse agonists) or activators of nuclear receptors, and small molecule inhibotors of carboxylic acid transporters as potential therapeutic agents.

Education

B.S., Chemistry, University of California, Los Angeles, 1974
Ph.D., Chemistry, Harvard University, 1977

Professional Experience

1977-78, Postdoctoral research, Harvard University
1978-83, Assistant Professor of Chemistry, Massachusetts Institute of Technology
1983-86, Associate Professor of Chemistry, Massachusetts Institute of Technology
1987-89, Associate Professor of Chemistry, Indiana University
1989-95, Professor of Chemistry, Indiana University
1995-97, Distinguished Professor of Chemistry, Indiana University
1997-2005, Warner Lambert/Parke Davis Professor of Chemistry, University of Michigan
2002-2004, Chair, Department of Chemistry, University of Michigan

Awards & Professional Activities

1982-86, Fellow of the Alfred P. Sloan Foundation
1992, Alan R. Day Award of the Philadelphia Organic Chemist's Club
1994, Arthur C. Cope Scholar Award, American Chemical Society
1996, ACS Akron Section Award 1996 Merit Award, National Institute of General MedicalSciences
1999, Distinguished Faculty Achievement Award, University ofMichigan
2002, Paul G. Gassman Distinguished Service Award, ACS Divisionof Organic Chemistry
2004, ACS Ernest Guenther Award in the Chemistry of NaturalProducts
2006, Fellow, American Association for the Advancement of Science
2009, Fellow, American Chemical Society

1990-93, Secretary-Treasurer, ACS Division of OrganicChemistry
1995, Chairman, ACS Division of Organic Chemistry
1990-02, Alternate Councilor, ACS Division of OrganicChemistry
1990-93, NIH Medicinal Chemistry Study Section, Member
1993-95, Chairman, NIH Medicinal Chemistry Study Section
1991-2002, Editorial Board, Organic Reactions
1995-present, Board of Directors, Organic Reactions
1992-2002, Editorial Board, Encyclopedia of Reagents for OrganicSynthesis
1993-2002, Editorial Board, Organic Syntheses
2003-present, Board of Directors, Organic Syntheses
1996-2002, Consulting Editorial Board, Tetrahedron
1999-present, Editorial Advisory Board, Organic Letters
1999-present, Associate Editor, Journal of the American Chemical Society
2005-present, Editorial Advisory Board, Chemical Biolgy and Drug Design
2005-present, Editorial Advisory Board, Beilstein Journal of Organic Chemistry
2007-2009, Editorial Advisory Board, Accounts of Chemical Research
2008-present, Scientific Advisory Board, Sandler Center for Basic Research in Parasitic Diseases, University of California San Francisco

Selected References

W. R. Roush, R. A. Hartz and D. J. Gustin, "Total Synthesis of Olivomycin A", J. Am. Chem. Soc., 1999, 121, 1990.

K. A. Scheidt, A. Tasaka, T. D. Bannister, M. D. Wendt, B. M. Savall, G. J. Fegley, and W. R. Roush, "Total Synthesis of (-)-Bafilomycin A1," J. Am. Chem. Soc., 2002, 124, 6981.

T. B. Durham, B. M. Savall, N. Blanchard, and W. R. Roush, "Total Synthesis of Formamicin," J. Am. Chem. Soc., 2004, 126, 9307.

D. J. Mergott, S. A. Frank, and W. R. Roush, "Total Synthesis of (-)-Spinosyn A via Transannular Diels-Alder Reaction/Ring Contraction Sequence," Proc. Natl. Acad. Sci. 2004, 101, 11955.

J. M. Tinsley and W. R. Roush, "Total Synthesis of Asimicin via Highly Stereoselective [3+2] Annulation Reactions of Substituted Allylsilanes," J. Am. Chem. Soc. 2005, 127, 10818.

P. Va and W. R. Roush, "Total Synthesis of Amphidinolide E," J. Am. Chem. Soc. 2006, 128, 15960.

M. Tortosa, N. A. Yakelis, and W. R. Roush, "Total Synthesis of Superstolide A," J. Am. Chem. Soc. 2008, 130, 2722.

J. R. Dunetz, L. D. Julian, J. Newcom and W. R. Roush, "Total Synthesis of (+)-Tedanolide and (+)-13-Deoxytedanolide," J. Am. Chem. Soc. 2008, 130, 16407.

J. Kister, A. C. DeBaille, R. Lira and W. R. Roush, "Stereoselective Synthesis of g-Substituted (Z)-Allylic Bornes via Kinetically Controlled Hydroboration of Allenes with 10-TMS-9-borabicyclo[3.3.2]decane," J. Am. Chem. Soc. 2009, 131, 14174.

M. Chen., D. H. Ess, and W. R. Roush, "Enantioselective Synthesis of (E)-d-Stannyl Homoallylic Alcohols via Aldehyde Allylboration Using a-Stannylallylborantes Generated by Allene Hydroboration Followed by a Highly Diastereoselective 1,3-Boratropic Shift," J. Am. Chem. Soc. 2010, 132, 7881.

Y. T. Chen, L. S. Brinen, I. D. Kerr, E. Hansell, P. S. Doyle, J. H. McKerrow, and W. R. Roush, “In Vitro and In Vivo Studies of the Trypanocidal Properties of WRR-483 against Trypanosoma cruzi”, PLoS Neglected Tropical Diseases 2010, 4, e825.

Y. Wang, N. Kumar, P. Nuhant, M. D. Cameron, M. A. Istrate, W. R. Roush, P. R. Griffin and T. P. Burris, "Identification of SR1078, a Synthetic Agnoist for the Orphan Nuclear Receptors RORa and RORg," ACS CHem. Biol. 2010, 5, 1029.

Links

Renowned University of Michigan Chemist Joins Scripps Florida Faculty

Roush Joins Scripps Florida