Gilbertson, Scott - University of Houston

个人简介

MD Anderson Professor Ph.D., University of Chicago, 1988 M.S., University of Michigan, 1982 B.S., University of Wisconsin-LaCrosse, 1979

研究领域

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.

近期论文

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“Synthesis and evaluation of dimeric derivatives of 5-HT2A receptor (5-HT2AR) antagonist M-100907,” Matthew J. Shashack, Kathryn A. Cunningham, Patricia K. Seitz, Andrew McGinnis, Thressa D. Smith, Cheryl S. Watson and Scott R. Gilbertson,* ACS Chemical Neuroscience, 2, 0000, (2011). “Design, synthesis and diversification of 3,5-substituted enone library,” Juhienah Khalaf, Maria E. Estrella-Jimenez, Matthew J. Shashack, Sharangdhar S. Phatak, Shuxing Zhang, and Scott R. Gilbertson* ACS Combinatorial Science, 13, 351, (2011). “Selective serotonin 5-HT2C receptor activation suppresses the reinforcing efficacy of cocaine and sucrose but differentially affects the incentive-salience value of cocaine- vs. sucrose-associated cues,” Kathryn A. Cunningham*, Robert G. Fox, Noelle C. Anastasio, Marcy J. Bubar, Sonja J. Stutz, F. Gerard Moeller, Scott R. Gilbertson, Sharon Rosenzweig-Lipson, Neuropharmacology, 513, (2011). “Pd-NHC Catalyzed Cyclopentannulation of Diazabicyclic Alkenes with ortho-aryl halides,” B. A. Bhanu Prasad, Alexander E. Buechele and Scott R. Gilbertson,* Organic Letters, 12, 5422, (2010). “Design, synthesis and diversification of 5,5-dimethyl cyclohexen-1,4-dione library,” Eric A. Tanifu and Scott R. Gilbertson,* J. Combi. Chem. 12, 318, (2010). “Testing efficacy and toxicity of adenylyl cyclase inhibitors against enteric pathogens during in vitro and in vivo models of infection,” Scott T. Moen, Carla A. Blumentritt, Terry M. Slater, Shilp D. Patel, Christopher B. Tutt, Maria E. Estrella-Jimenez, Jennifer Pawlik, Laurie Sower, Vsevolod L. Popov, Catherine H. Schein, Scott R. Gilbertson, Johnny W. Petersona, Alfredo G. Torres,* Infection and Immunity, 78, 1740, (2010). “The One-Pot Synthesis of Unsymmetrical N-heterocyclic Carbene Ligands From N-(2-iodoethyl)arylamine salts,” B. A. Bhanu Prasad and Scott R. Gilbertson,* Organic Lett. 11, 3710, (2009). “Novel Pyridopyrimidine Derivatives as Inhibitors of Stable Toxin a Induced cGMP Synthesis,” Eric A. Tanifum, Alexander Y. Kots, Byung-Kwon Choi, Ferid Murad, and Scott R. Gilbertson,* Bioorg. Med. Chem. Lett. 23, 3067, (2009). “Chemical genetic screening of KRAS-based synthetic lethal inhibitors for pancreatic cancer,” Zhenyu Ji, Fang C. Mei, Pedro L. Lory, Scott R. Gilbertson, Yijun Chen and Xiaodong Cheng,* Frontiers in Bioscience, 14, 2904-2910, (2009). “Preparation of a library of unsymmetrical ureas based on 8-azabicyclo[3.2.1]octane scaffold,” Anton Agarkov and Scott R. Gilbertson,* J. Combi. Chem. 655, (2008). “Novel inhibitors of cyclic nucleotide synthesis: application for treatment of diarrhea,” Alexander Y. Kots, Byung-Kwon Choi, Maria E. Estrella-Jimenez, Cirle A. Warren, Scott R. Gilbertson, Richard L. Guerrant and Ferid Murad,* PNAS 105, 8440, (2008). “Synthesis and Screening of Small Molecule Inhibitors of Anthrax Edema Factor,” Maria Estrella Jimenez, Kathryn Bush, Jennifer Pawlik, Laurie Sower, Johnny W. Peterson, and Scott R. Gilbertson,* Bioorg. Med. Chem. Lett. 22, 4215, (2008). A review of “Small-Molecule Inhibitors of Protein Geranylgeranyltransferase Type I,” Subhasis De and Scott R. Gilbertson,* ChemTracts, 20, 210, (2008). “Plasmodium Food Vacuole Plasmepsins are Activated by Falcipains,” Mark E. Drew, Ritu Banerjee, Eric W. Uffman, Scott R. Gilbertson, Philip J. Rosenthal, Daniel E. Goldberg,* J. Biol. Chem. 12870, (2008). “Substrate specificity and screening of the integral membrane protease Pla,” Anton Agarkov, Sadhana Chauhan, Pedro J. Lory, Scott R. Gilbertson* and Vladimir L. Motin, Bioorg. Med. Chem. Lett., 427, (2008). “Synthesis and screening of 3-substituted thioxanthen-9-one-10,10 dioxides,” Pedro M. J. Lory, Maria E. Estrella-Jimenez, Matthew J. Shashack, Ganesh L. Lokesh, Amarnath Natarajan and Scott R. Gilbertson,* Bioorg. Med. Chem. Lett. 21, 5940, (2007). “Rhodium Catalyzed Synthesis of Eight-Membered Rings,” Brenton DeBoef Richard Counts and Scott R. Gilbertson,* J. Org. Chem. 72, 799, (2007). “An expedient route to 3-chlorothioxanthen-9-one-10,10-dioxide and derivation by palladium catalyzed coupling,” Pedro M. J. Lory, Anton Agarkov and Scott. R. Gilbertson,* Synlett, 18, 3045, (2006). A review of “The Liebeskind-Srogl cross-coupling reaction and its synthetic application,” Pedro Lory and Scott G. Gilbertson,* ChemTracts, 18, 569, (2006). “Synthesis of Phosphine Containing Amino Acids: Utilization of Peptide Synthesis in Ligand Design,” Anton Agarkov, Scott Greenfield, Dejian Xie, Robert Pawlick, Gale Starkey and Scott R. Gilbertson,* Biopolymers, 84, 48, (2006).