Browsing by Author "Zhao, Jielu"
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- A descriptive study of the centralized system of higher education in ChinaZhao, Jielu (Virginia Tech, 1994)This study has two purposes: (1) to document and analyze the centralization phenomena in China's higher education system and (2) to make suggestions to improve or modify the centralization of China's higher education system in light of the documentation and analysis. A major outcome of this study is an analysis of telephone interviews and secondary documents, and four recommendations are derived from this analysis. In this study four research questions have been investigated: (1) What relationship exists between the government and individual colleges or universities? What should this relationship be? (2) What kind of relationship exists between the Party committee and the university administration, especially the relationship between the university president and Party committee? What should this relationship be? (3) How much autonomy should the colleges and universities possess? (4) How should higher education institutions move from the centralization planning economy and adapt themselves to the market economy? Two methods have been employed in this study: secondary document analysis and telephone interviewing. The secondary analysis consists of information collection in both Chinese and American libraries, information evaluation, categorization, and analysis. The telephone interviewing has been used to strengthen secondary analysis. The interviews were conducted with 15 Chinese scholars who were studying in the U.S. at the time and who have either worked in China's higher education system for more than ten years or have assumed some administrative responsibilities above the department level in that system. The major findings of the telephone interviews and secondary analysis lead to the conclusion that the higher education system in present China is highly centralized and, according to the consensus viewpoint, should be decentralized in light of the four recommendations made in this study.
- Design, Syntheses and Biological Activities of Paclitaxel AnalogsZhao, Jielu (Virginia Tech, 2011-01-31)The conformation of paclitaxel in the bound state on the protein has been proposed to be the T-taxol conformation, and paclitaxel analogs constrained to the T-taxol conformation proved to be significantly more active than paclitaxel in both cytotoxicity and tubulin polymerization assays, thus validating the T-taxol conformation as the tubulin-binding conformation. In this work, eight compounds containing an aza-tricyclic moiety as a mimic of the baccatin core of paclitaxel have been designed and synthesized as water-soluble simplified paclitaxel analogs, among which 3.50-3.52 and 3.55 were conformationally constrained analogs designed to bind to the paclitaxel binding site of tubulin, based on their similarity to the T-taxol conformation. The open-chain analogs 3.41-3.43 and 3.57 and the bridged analogs 3.50-3.52 and 3.55 were evaluated for their antiproliferative activities against the A2780 cell lines. Analogs 3.50-3.52 and 3.55 which were designed to adopt the T-taxol conformation showed similar antiproliferative activities compared to their open-chain counterparts. They were all much less active than paclitaxel. In the second project, a series of paclitaxel analogs with various thio-containing linkers at C-2′ and C-7 positions were designed and synthesized in our lab. These analogs were attached to the surfaces of gold nanoparticles by CytImmune Sciences for the development of mutifunctional tumor-targeting agents. The native analogs and the gold bound analogs were evaluated for their antiproliferative activities against the A2780 cell line. All the compounds tested showed comparable or better activities than paclitaxel. Stability studies were performed for selected analogs in hydrolysis buffer, which showed that the analogs released paclitaxel in buffer over time. In the third project, the synthesis of a conformationally constrained paclitaxel analog which was designed to mimic the REDOR-taxol conformation was attempted. Two synthetic routes were tried and significant progress was made toward the synthesis of the conformationally constrained analog. However, both of the current synthetic routes failed to produce the key intermediate that would serve as the precursor for a ring-closing metathesis reaction to furnish the macrocyclic ring.
- Thiolated paclitaxels for reaction with gold nanoparticles as drug delivery agents(United States Patent and Trademark Office, 2013-10-15)Thioloated taxane derivatives are linked to colloidal metal particles such as gold nanoparticles for use as antitumor agents. The antitumor agents may be targeted to tumors.