Global ETD Search
Search theses and dissertations gathered from participating repositories worldwide. Every result links back to the library that holds it. No account is needed.
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Showing 1 to 20 of 21 for “"self-immolative"”.
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Development of Novel Self-Immolative Linkers based on Fragmentation and Cyclisation Reactions for Targeted Therapeutic Applications
La terapia dirigida se ha erigido a lo largo de los últimos años como una de las estrategias más prometedoras para el tratamiento del cáncer. Estos sistemas consisten en una molécula con una alta afinidad y selectividad hacia una diana presente en células cancerosas, conjugada a fármacos …
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Single-Payload Bioconjugation to Native Antibodies And A General Method for the Self-Immolative Release of Amide-Containing Molecules
… the method to be compatible with commonly used self-immolative systems. The sulphonamide sulfamethizole was successfully released, however, the linkage proved instable preventing further exploitation of the method for sulphonamides. Urea and thioamide release was also attempted but proved …
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Synthesis and Characterization of Redox-Sensitive Polymer and Prodrug for Targeted Drug Delivery
… successful syntheses of l-RSP, a redox-sensitive self-immolative polymer, and DNS-SN38, thiol-sensitive SN-38 prodrug, as potential candidates for targeted drug delivery platforms. By covalently conjugating a redox-trigger (p-nitrobenzyl alcohol) and self-immolative linker (p-hydroxybenzyl …
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Synthesis of Small Molecule and Polymeric Systems for the Controlled Release of Sulfur Signaling Molecules
… the 1,6-benzyl elimination reaction (or self-immolative reaction) to facilitate the release of a persulfide (R–SSH) from a small molecule prodrug platform as well as a separate system that releases COS/H₂S from a polymer. The self-immolative persulfide prodrug was designed to be …
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The Development of Peroxide-Responsive Arylboronic Acids for Antibody-Drug Conjugates and Small-Molecule Prodrugs
… peroxide, and when combined with a suitable self-immolative aryl ring, can subsequently undergo spontaneous 1,6-elimination to release a free drug. Hence, initial studies evaluated a panel of model linkers with a fluorescent reporter molecule and confirmed the linker reactivity with peroxide …
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Tumor-Specific STING Agonist Synthesis via a Two-Component Prodrug System
… ronments. Caging one of the reactants with a self-immolative 𝛽-glucuronide moiety resulted in a two-component prodrug system that near-exclusively formed the active compounds in tumors overexpressing 𝛽-glucuronidase. These results exemplify the use of small-molecule recognition for on-site …
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Small Molecule and Macromolecular Donors of Reactive Sulfur Species: Insights into Reactivity and Therapeutic Potential
… elimination reaction (sometimes called self-immolation) to trigger release of a persulfide from a small molecule, polymeric, or peptide-based prodrug platform. Importantly, the first self-immolative small molecule persulfide prodrug (termed BDP-NAC) was designed to respond to reactive …
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Direct Liquid Chromatographic Separation of Enantiomers of Phthalides, Phthalimidines and Related Compounds on Chiral Stationary Phases
… enantiomerically enriched products owing to the self-immolative transfer of chirality from central to axial, back to central chirality. Factors affecting this process are discussed.
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Poly(ethyl glyoxylate) Solid-Core Particles for Drug Delivery
… of cargo. Polymeric nanotechnology containing “self-immolative polymers” looks to alleviate the reliance on high concentrations of stimuli by undergoing complete end-to-end depolymerization via a single stimulus-mediated reaction of an end-cap. Herein, NPs were developed using poly(ethyl …
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Synthesis of diene ligands with H-bonding capabilities for bioimaging applications
… investigated. The synthesis of bioprobes with self-immolative linkers that also contain both fluorophores and tricarbonyliron complexes and a study of their enzymatic cleavage reactions is also described. The reaction of an electrophilic cyclohexadienyliron(1+) complex with …
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Design and synthesis of indole-based analogues of OXi8006 as inhibitors of tubulin polymerization and their incorporation as payloads in drug-linker constructs.
… of an attachment group, a dipeptide linker, a self-immolative spacer, and the payload.
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Design and synthesis of benzosuberene and tetracyclic-based molecules inspired by natural products as inhibitors of tubulin polymerization and preparation of drug-linker constructs to facilitate tumor selective targeted delivery.
… phenolic payloads, constructs with alternative self-immolative spacers were prepared and evaluated for their release.
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Synthetic Degradable Polymer Systems for Drug Delivery
… the preparation and study of dual-responsive, self-immolative polyion complexes (PICs) nanoparticles. Depolymerization of the PICs using two complementary stimuli was demonstrated and the cytotoxicity of the PICs was investigated, followed by preliminary investigations of protein loading. …
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NOVEL STRATEGIES FOR IMPROVING THE PHARMACOLOGICAL PROPERTIES OF PLATINUM-ACRIDINE ANTICANCER AGENTS
… and/or NMR techniques: (i) a platinum-assisted, self-immolative ester cleavage in a low-chloride environment, and (ii) enzymatic cleavage by human carboxylesterase-2 (hCES-2). Highly efficient amide coupling reactions in platinum complexes were also developed. This modular approach can be used to …
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Design of smart linkers and their applications in controlled-release drug delivery systems
… the use of the Grob fragmentation to design ‘self-immolative’ linkers for controlled drug release. Altough the reaction mechanism is well know and presents several synthethic application, no biological application has been described to date. The screening of different substrates allowed the …
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Dual Delivery Systems Based On Polyamine Analog Benspm As Prodrug And Gene Delivery Vectors
… incorporated bis(2-hydroxyethyl) disulfide as a self-immolative linker to synthesize polymer prodrugs of BENSpm (DSS-BEN). The proposed mechanism of BENSpm release from DSS-BEN contains two steps: disulfide bond is first cleaved in the reducing intracellular space, then the intermediate further …
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Mechanochemical Reaction Development for Addition, Elimination, and Isomerization
… hydrogen fluoride has applications in self-immolative polymers, remodeled siloxanes, and degradable polymers. The responsive, in situ generation of HF in materials therefore holds promise for new classes of adaptive material systems. We achieve the mechanochemically coupled generation …
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