Scott Gilbertson
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Scott Gilbertson
MD Anderson Professor
Ph.D., University of Chicago, 1988
M.S., University of Michigan, 1982
B.S., University of Wisconsin-LaCrosse, 1979
Department of Chemistry
University of Houston
Houston, Texas 77204-5003
Office: 5027 - SERC
Phone: 832.842.8821
srgilbertson@uh.edu
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| Our research is centered on the development of new synthetic methods
and the utilization of synthetic chemistry for the study of important
biological and medical problems. The projects in our laboratory range
from the development of new methods in organic synthesis and the total
synthesis of biologically important natural products to medicinal
chemistry around leads compounds. We do a significant amount of work in
collaboration with biomedical researchers in the Houston/Galveston area.
Many of our projects provide us with a unique opportunity to test the
biological activity of our compounds and make modifications to improve
activity or test important biological principles. Some of the projects
we are currently working on are:
Development of Chemistry for Small Molecule Library Synthesis
Combinatorial chemistry is a valuable tool for the discovery of
new drug candidates. The ability to synthesize hundreds of compounds for
screening is a useful complement to rational drug design. We are
developing general approaches for the synthesis of a variety of organic
structures. These molecules will then be screened for biological
activity often in collaboration with colleagues. Some of the biological
areas we are developing libraries for are the investigation of
anti-viral, anti-cancer, anti-malaria compounds and inhibitors of
anthrax edema factor.
Total Synthesis and Medicinal Chemistry of
Biologically Important Natural Products We have begun the total synthesis of a number of natural products
that possess important biological activity. Our approaches are designed
to not only provide the natural product but also to allow for
significant modification around a target's basic scaffold. Two systems
we are currently working on are Salvinorin A and Dysiherbaine.
Rhodium Catalyzed Synthesis of Medium Sized Rings
In the area of synthetic methods development, we are working on
new reagents to form multiple carbon-carbon bonds in one reaction. One
example of such a reaction is a rhodium catalyzed [4+2+2] reaction we
have invented. In this case a dieneyne and an alkyne are combined, under
rhodium catalysis, to form a new cyclooctatriene. This chemistry is
currently being developed for other unsaturated systems and the
synthesis of natural products including asteriscanolide.
Peptide Based Catalysts Much is known about the three-dimensional structure of peptides.
In one project we are using the structural features of these molecules
in the de novo design of unnatural enzymes. By designing and building
peptides that possess the ability to bind catalytically active
transition metals we are developing new types of catalysts. We are
taking two approaches to this problem. One method is to synthesize
unnatural amino acids, and then by solution phase, solid phase or
combinatorial synthesis techniques, build peptides of moderate length.
The other route is via the modification of naturally occurring proteins.
Proteins that contain unnatural metals have a number of potential uses.
In addition to being entirely new types of catalysts, they should be of
use as radio-imaging agents, as site-specific DNA cleavage agents and
as catalytic enzyme inhibitors.
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