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Medicinal-Pharmaceutical Chemistry Commons

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Full-Text Articles in Medicinal-Pharmaceutical Chemistry

Synthesis, Self-Assembly, And Immunological Activity Of Α-Galactose-Functionalized Dendron–Lipid Amphiphiles, John Trant, Namrata Jain, D. M. Mazzuca, J Trevor Mcintosh, Bo Fan, S M Mansour Haeryfar, Sebastien Lecommandoux, Elizabeth Gillies Sep 2016

Synthesis, Self-Assembly, And Immunological Activity Of Α-Galactose-Functionalized Dendron–Lipid Amphiphiles, John Trant, Namrata Jain, D. M. Mazzuca, J Trevor Mcintosh, Bo Fan, S M Mansour Haeryfar, Sebastien Lecommandoux, Elizabeth Gillies

Chemistry Publications

Nanoassemblies presenting multivalent displays of biologically active carbohydrates are of significant interest for a wide array of biomedical applications ranging from drug delivery to immunotherapy. In this study, glycodendronlipid hybrids were developed as a new and tunable class of dendritic amphiphiles. A modular synthesis was used to prepare dendronlipid hybrids comprising distearylglycerol and 0 through 4th generation polyester dendrons with peripheral protected amines. Following deprotection of the amines, an isothiocyanate derivative of C-linked α-galactose (α-Gal) was conjugated to the dendron peripheries, affording amphiphiles with 1 to 16 α-Gal moieties. Self-assembly in water through a ...


The Design And Synthesis Of Ghrelin Analogues As Non‐Invasive Ghs‐R1a Imaging Probes, Carlie L. Charlton Feb 2016

The Design And Synthesis Of Ghrelin Analogues As Non‐Invasive Ghs‐R1a Imaging Probes, Carlie L. Charlton

Electronic Thesis and Dissertation Repository

The field of molecular imaging is constantly growing and evolving in order to provide the best possible healthcare for patients in various stages of disease and therapy. Molecular imaging aims to locate specific markers of disease by selectively targeting the markers of interest with high selectivity and visualizing the accumulation using external detection. The growth hormone secretagogue receptor-1a (GHS-R1a) has been shown to be involved in various important biological functions such as energy homeostasis and cardiac contractility. GHS-R1a has shown involvement in proliferation, migration and cell invasion of specific cancer subtypes. Therefore, targeting GHS-R1a is an important marker of different ...


Design, Synthesis, And Reactivity Of Bimetallic Complexes Of Dimethylplatinum(Ii) Containing Ditopic Ligands, Matthew S. Mccready Apr 2015

Design, Synthesis, And Reactivity Of Bimetallic Complexes Of Dimethylplatinum(Ii) Containing Ditopic Ligands, Matthew S. Mccready

Electronic Thesis and Dissertation Repository

This thesis describes a study of monometallic and bimetallic dimethylplatinum(II) complexes containing ditopic nitrogen donor ligands. This work details the design and synthesis of side-to-side and cofacial arranged ligands and their respective coordination chemistry. The study of the synthesis, characterization and reaction mechanisms of the various dimethylplatinum(II) complexes is outlined in detail with special emphasis focused on the reactivity of the complexes towards oxidative addition.

The ditopic ligand 6-dppd, 1,4-di(2-pyridyl)-5,6,7,8,9,10-hexahydrocycloocta[d]pyridazine, was observed to coordinate only a single equivalent of a platinum(II) center. The inability to coordinate a ...


Development Of A Gallium-Containing One-Bead One-Compound Peptide Library For The Discovery Of New Molecular Imaging Probes, Fernanda C. Bononi Aug 2014

Development Of A Gallium-Containing One-Bead One-Compound Peptide Library For The Discovery Of New Molecular Imaging Probes, Fernanda C. Bononi

Electronic Thesis and Dissertation Repository

An eight amino acid one-bead one-compound (OBOC) peptide library, containing a gallium-DOTA complex, was developed in an attempt to overcome common issues associated with the later addition of radionuclides to peptide chains of imaging probes. The further addition of a radionuclide often changes the binding properties of a peptide, as it adds bulk, and possibly charges. MALDI (matrix-assisted laser desorption ionization) tandem mass spectrometry was determined to be the method of choice in order to deconvolute gallium-containing peptide sequences. The library obtained was screened against the breast cancer cell lines MDA-MB-231 and MCF-7. Positive beads were isolated and sequences were ...