Discovery of Novel Phthalazinone Derivatives as Potent Ectonucleotide Pyrophosphatase/Phosphodie sterase-1 (ENPP1) Inhibitor for Cancer Immunotherapy
- 주제(키워드) ectonucleotide pyrophosphatase/phosphodiesterase 1 (ENPP1) , 2’ , 3’-cyclic guanosine monophosphate–adenosine monophosphate (cGAMP) , cyclic guanosine monophosphate–adenosine monophosphate synthase–stimulator of interferon genes (cGAS–STING) , innate immune system , phthalazinone inhibitor
- 주제(DDC) 547
- 발행기관 아주대학교
- 지도교수 최준원
- 발행년도 2023
- 학위수여년월 2023. 2
- 학위명 석사
- 학과 및 전공 일반대학원 분자과학기술학과
- 실제URI http://www.dcollection.net/handler/ajou/000000032656
- 본문언어 한국어
- 저작권 아주대학교 논문은 저작권에 의해 보호받습니다.
목차
1. Introduction 1
1.1. Cancer immunotherapy and the cGAS–STING pathway 1
1.2. ENPP1 as a therapeutic target in cancer 3
1.3. ENPP1 inhibitors for cancer immunotherapy 4
2. Results and Discussion 7
2.1. Synthesis of the phthalazinone derivatives 7
2.2. Structure-activity relationship 13
2.3. Biological evaluation 17
2.4. Docking studies 21
2.5. CYP inhibition, metabolic stability, and PK profiling 21
2.6. In vivo efficacy 23
3. Conclusions 24
4. Experimental Section 25
4.1. General information 25
4.2. Synthetic procedure 26
5. References 134
6. 1H and 13C NMR spectra 144
