Synthesis and biological evaluation of PSMA-targeted compounds for diagnosis and treatment = 진단 및 치료용 PSMA 표적 화합물의 합성 및 생물학적 평가

목차 (Table of Contents)

• Part I 1
• Abstract 2
• Abbreviation 4
• 1. Introduction 5
• 1.1. Prostate cancer 5
• 1.2. Prostate-specific membrane antigen (PSMA) 6
• 1.2.1 Discovery and development of PSMA-targeted inhibitors 7
• 1.2.2. PSMA-targeted optical imaging 10
• 2. Results and Discussion 12
• 2.1. Synthesis 12
• 2.1.1. PSMA-binding moiety 12
• 2.1.2. PSMA-inhibitory assay 14
• 2.2. In vitro biochemical evaluation 15
• 2.2.1. Cell uptake assay 16
• 3. Conclusion 18
• 4. Experimental Section 20
• 4.1. General 20
• 4.2. Chemistry 22
• 4.3. Biological Experiments 28
• Part II 29
• Abstract 30
• 1. Introduction 32
• 1.1. Peptide-drug conjugate (PDC) 32
• 1.2. Mechanism of Peptide-drug conjugate 33
• 1.3. Discovery and development of toxic substances in cancer cells 34
• 1.4. Conjugation of peptides and cytotoxic structures 35
• 2. Results and Discussion 36
• 2.1. Synthesis 36
• 2.1.1. Synthesis of PSMA binding moiety 36
• 2.1.2. Synthesis of cytotoxic moiety of Peptide-Drug conjugate 37
• 2.1.3 Synthesis of Peptide-Drug Conjugate targeting PSMA 38
• 3. Conclusion 39
• 4. Experimental Section 40
• 4.1. General 40
• 4.2. Chemistry 42
• 4.3. In silico modeling method 47
• 국문 초록 51
• 5. References 55
• Appendix 60
• List of appendix figures 60
• 감사의 글 77