I am interested in the design of DNA binding ligands which are including DNA minor groove binders and G-quadruplex stabilizing agents. Certain natural products, distamycin and belomycin are considered as models for designing new DNA binding agents. A variety of DNA binding ligands were synthesized and accordingly characterized by different bioassays. In the series of azo-pyrrole-polyamide, it showed slight DNA binding affinity but has the properties of DNA photo-cleavage and recognition of mixed sequence. The thiophene series showed strong binding ability for duplex DNA. Bithiophene series showed a remarkable binding affinity to duplex DNA which is compatible to natural products netropsin and distamycin. The pyridodicarboxamide series remain intramolecular hydrogen bonding with poor preferences for duplexes DNA even though they stabilized quadruplex DNA. The bithiophene-bipyrimidine compound binds to specific hexanucleotide sequence 5¡¦-AAGCTT-3¡¦ and acts as an unfused quadruplex stabilization ligand. In the quinoline series, the combination of quinoline and methylpyrrole polyamide proves the attenuation effect for quadruplexes stabilization which provides a novel strategy for development of quadruplex binding logands. In this study, several series of small molecules for DNA binding have been successfully synthesized and proved to interact with DNA secondary structures according to the particular properties of themselves.

Lithium iron phosphate (LiFePO4) is prepared by hydrothermal process using Fe(III) as precursor and pyrrole as an efficient reducing agent. The Fe(III) precursor in the system reacts with pyrrole to generate polypyrrole (PPy) and reduce Fe(III) to Fe(II). The different molar ratio Fe(III) polymerize different content of PPy and PPy can also be a carbon source for further calcination. The structural and morphological properties of LiFePO4 powder were characterized by X-ray diffraction (XRD), scanning electron microscope (SEM), and a transmission electron microscope (TEM). The XRD and TEM results demonstrate that LiFePO4 powder has an orthorhombic olivine-type structure with a space group of Pnma. The SEM and TEM results show that the particle size of LiFePO4 is around 200 nm and a layer of carbon coats on LiFePO4. The chemical composition of the LiFePO4 powder was characterized by elemental analysis (EA) and inductively coupled plasma/mass spectroscopy (ICP/MS). Raman and X-ray photoelectron spectroscopy (XPS) results indicate that pyrrole as a reducing agent reduces and prevents the formation of Fe(III) impurity and the resulting PPy plays a role as carbon source. Among the synthesized cathode materials, LiFePO4 synthesized using 5% molar ratio of Fe(III) and subsequent calcinations of 600 ¢XC shows the best electrochemical property with an discharge capacity of 160 mAhg−1 close to its theoretical capacity 170 mAh g−1 at 0.2 C rate. Using 10% molar ratio of Fe(III), and the discharge capacity of LiFePO4 at 10 C rate reaches 106 mAhg−1.

Synthetic netropsin analogs of the thiophene and pyridine, induce the netropsin analogs binding DNA from A-T base pair change to G-C base pair. Moreover, dendritic electrostatic groups have bulky conformation, which induce the netropsin analogs binding DNA to major groove.

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Despite progress in the metal-catalyzed synthesis of aromatic heterocycles, annulation routes towards 6-membered heterocycles remain underdeveloped. Specifically, routes towards pyridines are rare in spite of the prevalence of this moiety in novel drug candidates. Our initial efforts towards pyridines featured oximes as competent nucleophiles in the intramolecular, 6-exo dig annulation of alkynes using Brønsted acid catalysis. Two of the oxidation states required for subsequent aromatization are contained within the oxime via loss of water. An extension of this chemistry is presented and discussed, and involves the intramolecular metal-catalyzed 6-endo dig annulation of analagous alkynyl-oximes. Additionally, the discovery of a 5-exo dig annulation of related systems is discussed.

Please read the abstract in the section 00front of this document / Dissertation (MSc (Chemistry))--University of Pretoria, 2006. / Chemistry / unrestricted

Despite progress in the metal-catalyzed synthesis of aromatic heterocycles, annulation routes towards 6-membered heterocycles remain underdeveloped. Specifically, routes towards pyridines are rare in spite of the prevalence of this moiety in novel drug candidates. Our initial efforts towards pyridines featured oximes as competent nucleophiles in the intramolecular, 6-exo dig annulation of alkynes using Brønsted acid catalysis. Two of the oxidation states required for subsequent aromatization are contained within the oxime via loss of water. An extension of this chemistry is presented and discussed, and involves the intramolecular metal-catalyzed 6-endo dig annulation of analagous alkynyl-oximes. Additionally, the discovery of a 5-exo dig annulation of related systems is discussed.

京都大学 / 0048 / 新制・課程博士 / 博士(理学) / 甲第20929号 / 理博第4381号 / 新制||理||1630(附属図書館) / 京都大学大学院理学研究科化学専攻 / (主査)教授 杉山 弘, 教授 三木 邦夫, 教授 秋山 芳展 / 学位規則第4条第1項該当 / Doctor of Science / Kyoto University / DGAM

京都大学 / 0048 / 新制・課程博士 / 博士(理学) / 甲第20951号 / 理博第4403号 / 新制||理||1632(附属図書館) / 京都大学大学院理学研究科化学専攻 / (主査)教授 大須賀 篤弘, 教授 丸岡 啓二, 教授 依光 英樹 / 学位規則第4条第1項該当 / Doctor of Science / Kyoto University / DGAM

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