| 摘要 | 第1-9页 |
| Abstract | 第9-26页 |
| Part Ⅰ:Design,Synthesis,Cytoselective Toxicity,and Structure-Activity Relationships(SAR) of Thiazolidinone Derivatives | 第26-117页 |
| Chapter 1.Introduction | 第26-40页 |
| The bottlenecks of anti-cancer drugs | 第26-27页 |
| Multidrug Resistance(MDR) and P-glycoprotein(P-gp) | 第27-30页 |
| Information of the lead compounds | 第30-32页 |
| Combinatorial chemistry and fluorous chemistry | 第32-34页 |
| Recent Advances in the Development of 4-Thiazolin-dinones | 第34-40页 |
| Chapter 2 Objectives | 第40-43页 |
| Chapter 3.Design,Synthesis and Cytoselective Anticancer Toxicity Assay of 4-Thiazolindinone Libraries | 第43-83页 |
| Design and synthesis of 2-arylimino-thiazolidin-4-ones(Library Ⅰ) | 第43-50页 |
| Design and synthesis 2-Arylimino-3-substituted-4-thiazolidinones(Library Ⅱ) | 第50-52页 |
| Design and synthesis of 2-aryl-substituted 4-thiazolin dinones using fluorous chemistry(Library Ⅲ and Ⅳ) | 第52-58页 |
| Cytoselective Anticancer Toxicity Assay of 4-Thiazo lindinone Libraries | 第58-62页 |
| Experimental section | 第62-83页 |
| Synthesis of 2-arylimino-thiazolidin-4-ones(library Ⅰ) | 第63-67页 |
| Synthesis of 2-arylimino-3-substituted-thiazolidin-4-ones(library Ⅱ) | 第67-69页 |
| General procedure for the library synthesis | 第69-70页 |
| General procedures for F-SPE: | 第70页 |
| Synthesis of 2-aryl-substituted-thiazolindin-4-ones(library Ⅲ and Ⅳ) | 第70-83页 |
| Chapter 4.Synthesis,SAR and Pharmacophore of Lead Optimization Thiazolidinone derivatives | 第83-97页 |
| Synthesis of the lead optimization library(Library Ⅴ) | 第83-84页 |
| Cytoselective Anticancer Toxicity Assay of lead optimization library | 第84-86页 |
| Time-dependent compound effects on cell proliferation and morphology | 第86页 |
| P-gp substrate and inhibitor pharmacophore modeling | 第86-89页 |
| Structure-activity relationship and pharmacophore modeling | 第89-91页 |
| Anticancer compounds are not Michael acceptors | 第91-92页 |
| Experimental section | 第92-97页 |
| Cells and Culture Conditions | 第95页 |
| Cytotoxicity assays | 第95-96页 |
| Time-dependent compound effects on cell proliferation and cell morphology | 第96页 |
| P-gp substrate pharmacophore modeling | 第96页 |
| Anti-cancer compound pharmacophore modeling | 第96-97页 |
| Chapter 5 Conclusion | 第97-102页 |
| References | 第102-117页 |
| Part Ⅱ:Design and synthesis of nanoparticles with better characterization and biocompatibility | 第117-209页 |
| Chapter 6 Introduction | 第117-131页 |
| Combinatorial approach for surface modification of nanoparticles | 第117-121页 |
| Surface characterization of nanoparticles by ~1H NMR | 第121-126页 |
| Multifunctionalization of nanoparticles | 第126-129页 |
| Objective | 第129-131页 |
| Chapter 7 Nano-combinatorial MWNTs library approach for discovering biocompatible nanocarriers | 第131-154页 |
| Introduction | 第131-132页 |
| Design of surface diversity for f-MWNT library | 第132-134页 |
| Library synthesis substantiated by thorough charac-terizations | 第134-141页 |
| Identification of protein evaders and associated SAR | 第141-144页 |
| Surface structure dependent cytotoxicity and immune response | 第144-146页 |
| Lead identification and SAR | 第146-148页 |
| Conclusion | 第148-149页 |
| Experimental section | 第149-154页 |
| Synthesis,purification and characterization of f-MWNT library | 第150-152页 |
| Protein binding assays | 第152-153页 |
| Cytotoxicity assay and quantification of NO release | 第153-154页 |
| Chapter 8 Characterization of organic molecules attached to GNPs by HRMAS NMR | 第154-170页 |
| Introduction | 第154-156页 |
| Synthesis of gold nanoparticles | 第156-158页 |
| Optimization of HRMAS NMR Parameters | 第158-161页 |
| ~1H HRMAS NMR | 第161-164页 |
| Two Dimensional HRMAS NMR of GNP | 第164-166页 |
| Conclusion | 第166页 |
| Experimental Section | 第166-170页 |
| Synthesis of the small molecules | 第167-168页 |
| Synthesis of gold nanoparticles | 第168-169页 |
| NMR experiments | 第169-170页 |
| Chapter 9.Synthesis of multifunctional GNPs by Combinatorial Approach | 第170-193页 |
| Introduction | 第170-171页 |
| Double functional GNPs with similar ligands(GNPs Ⅰ and Ⅱ) | 第171-174页 |
| Double functional GNPs with FITC and FA(GNPs Ⅲ) | 第174-177页 |
| Synthesis of double functional GNP library | 第177-179页 |
| Expermental section | 第179-180页 |
| Synthesis of double functional GNPs Ⅰ and Ⅱ | 第180-182页 |
| Synthesis of double functional GNPs Ⅲ | 第182-185页 |
| Synthesis of GNPs library | 第185-193页 |
| Chapter 10 Conclusion | 第193-195页 |
| References | 第195-209页 |
| Appendix | 第209-233页 |
| Acknowledgement | 第233-234页 |
| Selected publications | 第234-236页 |
| 学位论文评阅及答辩情况表 | 第236页 |
