文摘
英文文摘
论文说明:Lists of Tables、Lists of Figures、Lists of Schemes、Lists of Abbreviations
声明
Part Ⅰ:Design,Synthesis,Cytoselective Toxicity,and Structure-Activity Relation-ships(SAR) of Thiazolidinone Derivatives
Chapter 1.Introduction
The bottlenecks of anti-cancer drugs
Multidrug Resistance (MDR) and P-glycoprotein(P-gp)
Information of the lead compounds
Combinatorial chemistry and fluorous chemistry
Recent Advances in the Development of 4-Thiazolin-dinones
Chapter 2 Objectives
Chapter 3.Design,Synthesis and Cytoselective Anticancer Toxicity Assay of 4-Thiazolindinone Libraries
Design and synthesis of 2-arylimino-thiazolidin-4-ones(Library Ⅰ)
Design and synthesis 2-Arylimino-3-substituted-4-thiazolidinones(Library Ⅱ)
Design and synthesis of 2-aryl-substituted 4-thiazolin dinones using fluorous chemistry(Library Ⅲ and Ⅳ)
Cytoselective Anticancer Toxicity Assay of 4-Thiazo lindinone Libraries
Experimental section
Chapter 4.Synthesis,SAR and Pharmacophore of Lead Optimization Thiazolidinone derivatives
Synthesis of the lead optimization library(Library Ⅴ)
Cytoselective Anticancer Toxicity Assay of lead optimization library
Time-dependent compound effects on cell proliferation and morphology
P-gP substrate and inhibitor pharmacophore modeling
Structure-activity relationship and pharmacophore modeling
Anticancer compounds are not Michael acceptors
Experimental section
Chapter 5 Conclusion
References
Part Ⅱ:Design and synthesis of nanoparticles with better characterization and biocompatibility
Chapter 6 Introduction
Combinatorial approach for surface modification of nanoparticles
Surface characterization of nanoparticles by 1H NMR
Multifunctionalization of nanoparticles
Objectives
Chapter 7 Nano-combinatorial MWNTs library approach for discovering biocompatible nanocarriers
Introduction
Design of surface diversity for f-MWNT library
Library synthesis substantiated by thorough charac-terizations
Identification of protein evaders and associated structure activity relationship (SAR)
Surface structure dependent cytotoxicity and immune response
Lead identification and SAR
Conclusion
Experimental section
Chapter 8 Characterization of organic molecules attached to GNPs by HRMAS NMR
Introduction
Synthesis of gold nanoparticles
Optimization of HRMAS NMR Parameters
1H HRMAS NMR
Two Dimensional HRMAS NMR of GNP
Conclusion
Experimental Section
Chapter 9.Synthesis of multifunctional GNPs by Combinatorial Approach
Introduction
Double functional GNPs with similar ligands
Double functional GNPs with FITC
Synthesis of double functional GNP library
Expermental section
Chapter 10 Conclusion
References
Appendix
致谢
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