Medicinal Chemistry Dissertations and Theses: Recent submissions
Now showing items 1-20 of 80
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STUDIES OF INTERACTIONS OF SMALL MOLECULES WITH MEMBRANES AND PROTEINS
(University of Kansas, 2019-12-31)The modern molecular understanding of biological systems relies on integration of principles, practices, and techniques from diverse fields such as molecular biology, biochemistry, and biophysics. This approach has provided ... -
Discovery of Novel Inhibitors of Cellular Efflux by High-Content Screening with a Fluorescent Mimic of Taxol
(University of Kansas, 2019-08-31)Fluorescence-based assays play key roles in drug discovery and development. These assays are widely used due to the widespread availability of fluorescent probes and highly sensitive detection platforms. This method is a ... -
Synthesis and Evaluation of Fluorescent Tools for Studies of Cancer Biology
(University of Kansas, 2019-08-31)A key enabling technology in biological sciences involves fluorescent probes. These probes are typically small molecules, proteins, or nucleic acids that either possess intrinsic fluorescence or are linked to a fluorophore ... -
Strategies for the Fluorine-Retentive Functionalization of Gem-Difluoroalkenes
(University of Kansas, 2019-05-31)Fluorination is an important strategy for perturbing the biophysical properties of compounds in medicinal chemistry. Specifically, fluorination modulates both the pharmacodynamic and pharmacokinetic properties of bioactive ... -
Studies of novel targeted drug delivery systems and molecular probes of cancer biology
(University of Kansas, 2019-05-31)Cancer is a complex family of diseases. As our understanding of cancer biology has improved, so has our ability to treat the pathology associated with this condition. Traditional anticancer therapeutics lack selectivity ... -
Investigation of the Phenyl Ring of Imidazoquinolines
(University of Kansas, 2018-05-31)The 1H-Imidazo-[4,5-c]quinolines are a class of compounds that are agonists towards Toll-like receptor 7 and 8 (TLR7/8). For example, Imiquimod and Resiquimod have been shown to act as vaccine adjuvants, enhancing ... -
A New Generation of Isoform Selective Hsp90 Inhibitors: Targeting the Cytosolic Hsp90 Isoforms
(University of Kansas, 2018-05-31)Heat shock protein 90 kDa (Hsp90) is a member of the molecular chaperone family of proteins that processes newly synthesized polypeptides into their three-dimensional and biologically active form. In addition, Hsp90 assists ... -
The Development of Organelle-localized Hsp90 Isoform-selective Inhibitors
(University of Kansas, 2017-12-31)Molecular chaperones are responsible for the maturation of nascent polypeptides and the re-maturation of denatured proteins. One chaperone family that has emerged as an attractive therapeutic target is the 90 kDa heat shock ... -
Exploration of Salvinorin A for the Development of Pain and Addiction Therapies
(University of Kansas, 2017-08-31)In the search for effective methods to mitigate the increasing rates of abuse and addiction of illicit substances, a variety of neurological pathways have been explored. Towards this goal of reducing drug abuse and ultimately ... -
I. Development of Bisamides as Kappa Opioid Receptor Agonists. II. Potency Enhancement of Sulfonamide-based Kappa Opioid Receptor Antagonists. III. Asymmetric Acyl Transfer Reactions Catalyzed by a Cyclic Peptide.
(University of Kansas, 2017-05-31)Development of Bisamides as Kappa Opioid Receptor Agonists. The structure-activity relationship (SAR) expansion was carried out on bisamides KOR agonists. Previous four-step linear synthetic route was replaced by Ugi ... -
Design and synthesis of cyclic analogs of the kappa opioid receptor antagonist arodyn
(University of Kansas, 2018-05-31)Opioid receptors are important therapeutic targets for mood disorders and pain. Kappa opioid receptor (KOR) antagonists have recently shown potential for treating drug addiction and depression. Arodyn (Ac[Phe1,2,3,Arg4,D-Ala8]Dyn ... -
Advances in Heterocyclic Synthesis through Ring Expansions and Flow Chemistry
(University of Kansas, 2018-05-31)This dissertation comprises three chapters, which focus on the development of new synthetic methodologies and the construction of a screening collection. An Application of the Schmidt Reaction: Construction of an Azasteroid ... -
Exploration of the Mechanisms of Adjuvanticity for Toll-like Receptor Agonists
(University of Kansas, 2017-08-31)Small-molecule agonists have been identified for Toll-like Receptors (TLR) 2, TLR4, TLR7 and TLR8 thus far, and chemotypes other than those of canonical ligands are yet to be explored for a number of innate immune receptors. ... -
The Development of Small Molecules that Modulate Molecular Chaperones Hsp90 and Hsp70
(University of Kansas, 2017-12-31)The heat shock proteins are a highly conserved protein family that are constitutively expressed and function as molecular chaperones. Molecular chaperones 90kDa Heat Shock Protein (Hsp90) and 70kDa Heat Shock Protein (Hsp70) ... -
Synthetic Strategies to Access Biologically Important Fluorinated Motifs: Fluoroalkenes and Difluoroketones
(University of Kansas, 2017-05-31)Fluorine plays an important role in drug design, because of some unique features imparted by fluorine. The incorporation of fluorine into small molecules can modulate molecular physicochemical properties, metabolic stability, ... -
Design and Synthesis of Functionally Selective Kappa Opioid Receptor Ligands
(University of Kansas, 2017-05-31)The ability of ligands to differentially regulate the activity of signaling pathways coupled to a receptor potentially enables researchers to optimize therapeutically relevant efficacies, while minimizing activity at ... -
Copper-Catalyzed Decarboxylative Trifluoromethylation Reactions
(University of Kansas, 2017-05-31)Trifluoromethanes play an important role in medicinal chemistry, and methods that enable the rapid synthesis of trifluoromethanes from common functional groups are essential for the synthesis of bioactive compounds. We ... -
An Improved Synthesis of the Pacific Blue Fluorophore and Fluorescence-based Studies of Receptor-Ligand Interactions
(University of Kansas, 2016-12-31)Early-stage drug discovery and chemical biology projects often use fluorescence-based assays to obtain information about biological interactions and cellular processes. However, many of the best and brightest fluorophores ... -
Unfolding the Hsp90 Foldasome: Structure-Activity Relationship Studies on EGCG and Development of Isoform-Selective Inhibitors
(University of Kansas, 2016-08-31)The 90 kDa heat shock proteins (Hsp90) are critical for the maintenance of cellular homeostasis and mitigate the effects of cellular stress and therefore, play an important role in cell survival. Hsp90, as a molecular ... -
SYNTHESIS AND PHENOTYPIC DISCOVERY OF MOLECULAR PROBES OF BIOLOGICAL SYSTEMS
(University of Kansas, 2015-12-31)The Peterson laboratory has had a long-standing interest in fluorescent probes of biological systems. My research in the Peterson group has focused on the design, synthesis, and biological evaluation of fluorescent small ...