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http://tdr.lib.ntu.edu.tw/jspui/handle/123456789/76782完整後設資料紀錄
| DC 欄位 | 值 | 語言 |
|---|---|---|
| dc.contributor.advisor | 陳基旺(Ji-Wang Chern) | |
| dc.contributor.author | Yi-Hsun Ho | en |
| dc.contributor.author | 何宜洵 | zh_TW |
| dc.date.accessioned | 2021-07-10T21:36:52Z | - |
| dc.date.available | 2021-07-10T21:36:52Z | - |
| dc.date.copyright | 2015-08-28 | |
| dc.date.issued | 2015 | |
| dc.date.submitted | 2015-08-10 | |
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| dc.identifier.uri | http://tdr.lib.ntu.edu.tw/jspui/handle/123456789/76782 | - |
| dc.description.abstract | The aim of this thesis is to develop quinazolinone derivatives as selective HDAC6 inhibitors for the potential treatment of glioblastoma.
In our previous study, a series of quinazolinone derivatives as HDAC6 inhibitors had been designed and synthesized which employed quinazolinone as core structure to serve as enzyme surface recognition group and connected with hydroxamic acid through benzyl linker. In this thesis, compound 1 was selected as a lead which displayed HDAC6 IC50 at 5 nM, 650-fold selectivity to HDAC6 versus HDAC1, and IC50 at 0.87 μM against brain cancer cell line. More modifications on quinazolin-2,4-dione and different length of linkers at 2-position were accomplished to improve the HDAC6 inhibitory activity and cytotoxicity. Furthermore, structural mimics of the tricyclic ring of Tubastatin A were also synthesized to explore the tolerance of rim region. From the results obtained from enzyme assay and cytotoxic assay, compound 5h with fluoride at ortho position of phenyl ring displayed enhanced IC50 at 0.15μM against brain cancer cell line. Removing phenyl ring at N-3 position of lead compound 1and modifying phenyl ring of quinazolin-2,4-dione core resulted in modest reduction against HDAC6 inhibitory activities and cytotoxicity. Among different lengths of linker at 2-position, compound 20 with benzyl linker displayed HDAC6 IC50 at 0.7 nM with 1700-fold selectivity to HDAC6 versus HDAC1 and IC50 at 0.83 μM against brain cancer cell line. In the final part, mimics of tricyclic core of Tubastatin A showed increased inhibitory activity against HDAC6, but only displayed cytotoxicity at micromolar range. With potent inhibitory activities against HDAC6 and brain cancer cell line, compound 5h and 20 may serve as leads for development of potential therapeutic agents against glioblastoma. | en |
| dc.description.provenance | Made available in DSpace on 2021-07-10T21:36:52Z (GMT). No. of bitstreams: 1 ntu-104-R02423021-1.pdf: 11443795 bytes, checksum: b2bc8d97471f023fd8712ceee0e11b9b (MD5) Previous issue date: 2015 | en |
| dc.description.tableofcontents | 中文摘要 i
Abstract ii List of Figures iv List of Tables v List of Schemes vi Chapter 1. Introduction 1.1 Malignant gliomas 1 1.2 Target therapies for GBM in clinical trials 2 1.3 Histone deacetylase (HDAC) and HDAC Inhibitors 5 Chapter 2. Design and Synthesis of N-1, N-3-Disubstituted Quinazolin-2, 4-dione Derivatives 2.1 Introduction and Rational Design 11 2.2 Chemistry results and Discussion 14 2.3 Biological Activity 15 2.4 Experimental Section 20 Chapter 3. Design and Synthesis of N-1-Substituted Quinazolin-2, 4-dione Derivatives 3.1 Introduction and Rational Design 44 3.2 Chemistry results and Discussion 45 3.3 Biological Activity 46 3.4 Experimental section 50 Chapter 4. Design and Synthesis of 2-Substituted Quinazolin-4-one Derivatives 4.1 Introduction and Rational Design 65 4.2 Chemistry results and Discussion 67 4.3 Biological Activity 70 4.4 Experimental Section 73 Chapter 5. Design and Synthesis of 2,3-Dihydroimidazo[1,2-c]quinazolin-5(6H)-one Derivatives 5.1 Introduction and Rational Design 83 5.2 Chemistry results and Discussion 84 5.3 Biological Activity 85 5.4 Experimental Section 87 Chapter 6. Conclusion References 97 | |
| dc.language.iso | en | |
| dc.subject | 第六亞型組蛋白? | zh_TW |
| dc.subject | 多形性膠質母細胞瘤 | zh_TW |
| dc.subject | glioblastoma | en |
| dc.subject | HDAC6 | en |
| dc.title | 設計與合成第六亞型組蛋白去乙醯酶抑制劑作為抗多形性膠質母細胞瘤之潛能藥物 | zh_TW |
| dc.title | Design and Synthesis of HDAC6 Selective Inhibitor as Potential Agent against Glioblastoma | en |
| dc.type | Thesis | |
| dc.date.schoolyear | 103-2 | |
| dc.description.degree | 碩士 | |
| dc.contributor.oralexamcommittee | 顧記華(Jih-Hwa Guh),忻凌偉(Ling-Wei Hsin),梁碧惠(Pi-Hui Liang),王光昭(Kuang-Chao Wang) | |
| dc.subject.keyword | 第六亞型組蛋白?,多形性膠質母細胞瘤, | zh_TW |
| dc.subject.keyword | HDAC6,glioblastoma, | en |
| dc.relation.page | 111 | |
| dc.rights.note | 未授權 | |
| dc.date.accepted | 2015-08-10 | |
| dc.contributor.author-college | 藥學專業學院 | zh_TW |
| dc.contributor.author-dept | 藥學研究所 | zh_TW |
| 顯示於系所單位： | 藥學系 | |
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