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Showing 1 to 20 of 266 for “"Pharmaceutical chemistry"”.
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Some potential chemotherapeutic agents derived from aralkyl ketones
Dissertation (Ph.D.)--University of Kansas, Pharmaceutical Chemistry, 1952.
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Synthesis of novel 5,6-disubstituted derivatives of uracil as potential drugs
… of Pharmacy in Hradec Králové Department of Pharmaceutical Chemistry and Pharmaceutical Analysis Candidate: Vu Lien Phuong Supervisors: PharmDr. Marta Kučerová, Ph.D. Tanja Bruun, M.Sc. (Pharm.) Prof. Jari Yli-Kauhaluoma Title of diploma thesis: Synthesis of novel 5,6-disubstituted …
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1. C-C Bond Formation via Soft Enolization and Umpolung-like Chemistry 2. Electrophilic Fluorination of Organozinc Reagents
… formation, soft enolization and Umpolung-like chemistry. The direct synthesis of 1,3-diketones and β-keto thioesters using in good yields and with wide substrate tolerance was possible using our soft enolization strategy using crude acyl chlorides. Another C-C bond strategy explored was an …
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Application of pharmaceutical technologies to improve the activity of cancer chemotherapeutic agents
… quality of life. In this dissertation, different pharmaceutical technology approaches, including nanotechnology and pharmaceutical chemistry, were utilized to improve the activity of chemotherapeutic agents. Docetaxel is a second generation taxane used as a single agent in breast cancer, non-small …
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Bioreactor design for scaleup of Catharanthus roseus hairy root cultures for production of indole alkaloids
C. roseus is the source of the important anticancer indole alkaloids, vincristine and vinblastine. Hairy root cultures are an attractive alternative for the production of plant derived secondary metabolites. C. roseus hairy root cultures were established in our laboratory by A. rhizogenes mediated …
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Target Based Design And Synthesis of Heterocycles in the Potential Treatment of Cancer and Opportunistic Infection
<p>Dose limiting toxicity and development of multidrug resistance by the tumors are the major limitations of current cancer chemotherapy. Microtubule targeting agents (MTAs) are a structurally diverse set of compounds that disrupt microtubule dynamics and exert their anticancer effect. Among the …
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Design and synthesis of 3-[N-(cyclopropylmethyl) amino]-7-(methoxy or hydroxy)-2, 2-dimethyl-1-tetralone analogs as potential opioid receptor antagonists
<p>A series of 3-aminotetralins were synthesized as potential opioid antagonists. Each proposed target compound was based on a 3-(mono- or dialkylamino )-7 -(hydroxy or methoxy)-2, 2-dimethyl-1-tetralone parent structure. Three synthetic schemes were developed utilizing the common intermediate, …
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Synthesis and biological studies of a fullerene-Taxol conjugate and fullerene-based transfection vectors
… therapy, MRI contrast agents, and radiopharmaceuticals. The first part of this work is dedicated to the development of a new application of C60 as a slow-release system for the liposome aerosol delivery of lipophilic chemotherapeutics to lung cancer. TaxolRTM (paclitaxel), one of the …
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Investigations of the biosynthesis of sparsomycin
The biosynthesis of the antitumor antibiotic, sparsomycin, produced by Streptomyces sparsogenes, has been investigated. Incorporation studies employing ($\sp{13}$C)-labeled precursors have shown that both L- and D-isomers of S-(methylthio)methyl-cysteine are specifically incorporated into the …
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Studies on complex pyridine alkaloids: Total synthesis of cystodytin J, diplamine, shermilamine B and of Micrococcin P1
Concise, efficient total syntheses of cystodytin J, diplamine and shermilamine B have been accomplished. These cytotoxic marine alkaloids display a novel pyridoacridine architecture that was readily assembled by a combination of two new processes developed in our laboratory: a pyridine-forming …
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Thermodynamic and kinetic investigation of chiral separations using polysaccharide stationary phases
… (Ph. D.)--Michigan State University. Dept. of Chemistry, 2010
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Target Based Design and Synthesis of Fused Pyrimidines in the Potential Treatment of Cancer and Opportunistic Infection
<p>This dissertation describes an introduction, background and research progress in the areas of agents designed as (a) selective <em>Pneumocystis jirovecii</em> dihydrofolate reductase (pjDHFR) inhibitors for pneumocystis pneumonia (PCP) infection; (b) inhibitors of microtubule polymerization and …
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Evaluation of antihistamines for in vitro antimalarial activity against Plasmodium falciparum
… Thank for all your assistance.My dearest Pharmaceutical Chemistry colleagues, Jaques Joubert, for your friendship and support and for always listening and Prof. Peter Eagles, your kindness, support and wise advice has given me strength when I needed it most. To my other School of Pharmacy …
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Syntheses, bioactivities and conformations of peptidomimetics containing 2,3-methanoamino acids
… acids are compatible with solid phase chemistry, although they are more sterically hindered than their corresponding natural amino acids. Anti-opiate activities, and proteolytic stabilities of the peptidomimetics were studied. The peptidomimetics were more active (in vivo) than the …
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An improved synthesis of the HDAC inhibitor trichostatin A
<p>Histone deacetylase inhibitors (HDIs) have found a wide variety of medicinal uses and are most noted for their specific apoptotic action towards cancer cells. Several hydroxamate HDIs have since been moved on to phase 1 and 2 clinical drug trials, with one having already been approved for …
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