Synthesis and biology of lithocholic acid C4 fluorine-containing sialyltransferase inhitors and benzoxazinone-related fluorescent probes.
碩士 === 國立中央大學 === 化學學系 === 103 === PartI. According to many researches, abnormal expression of the sialyltransferase has been found to actually connect with many cancers. Therefore, purposes and objectives of this study are making effort to develop effective sialyltransferase inhibitors and regulate...
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ndltd-TW-103NCU050650802019-05-15T22:08:46Z http://ndltd.ncl.edu.tw/handle/6ua4tv Synthesis and biology of lithocholic acid C4 fluorine-containing sialyltransferase inhitors and benzoxazinone-related fluorescent probes. 石膽酸C4含氟唾液酸轉移酶抑制劑和苯並惡嗪酮相關的螢光探針之合成及生物研究 Ming-Xin Liu 劉明鑫 碩士 國立中央大學 化學學系 103 PartI. According to many researches, abnormal expression of the sialyltransferase has been found to actually connect with many cancers. Therefore, purposes and objectives of this study are making effort to develop effective sialyltransferase inhibitors and regulate the level of sialyltransferase expression.In the thesis, the main structure of our compounds are lithocholic acid. We used high efficient and selective reagent─Selectfluor to add a fluorine atom at the C4 position as modification, and we synthesized fluorinated compound of Lith-O-Asp-NBD as effective anti-cancer compound further.Through MTT assay and Wound healing assay experiment to discuss fluorinated compound’s influence on biologically activity. Interestingly, We found that compounds JO-5b, JO-13a, JO-13b possess potent anti-metastasis ability. PartII. Fluorescent labeling has the advantage of high sensitivity and good selectivity for the use in a wide range of applications. In recent years, novel molecular imaging agents were developed for the use of clinical translation through early lesion detection, molecular targeted therapy, therapeutic monitoring, and the development of new anti-cancer drugs. This action significantly improves diagnosis and therapy in patients with breast cancer metastasis. In this thesis, the main structure of our compounds is benzoxazinone. We modified its functional group to explore the relationship between structure and fluorescent quantum yield of molecular probes. Through analysis of the optical property, we found that Jo-35 has the highest quantum yield (Φ = 0.39) compared to that of others. Intramolecular hydrogen bond was confirmed in the skeleton between oxygen atom and amino group of the benzene ring. Molecular probes drop the fluorescent property if the intramolecular hydrogen bond is absent due to replacement of the amino group by other atom and/or moiety. Wen-Shan Li Dui-Ren Hou 李文山 侯敦仁 2015 學位論文 ; thesis 168 zh-TW |
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碩士 === 國立中央大學 === 化學學系 === 103 === PartI.
According to many researches, abnormal expression of the sialyltransferase has been found to actually connect with many cancers. Therefore, purposes and objectives of this study are making effort to develop effective sialyltransferase inhibitors and regulate the level of sialyltransferase expression.In the thesis, the main structure of our compounds are lithocholic acid. We used high efficient and selective reagent─Selectfluor to add a fluorine atom at the C4 position as modification, and we synthesized fluorinated compound of Lith-O-Asp-NBD as effective anti-cancer compound further.Through MTT assay and Wound healing assay experiment to discuss fluorinated compound’s influence on biologically activity. Interestingly, We found that compounds JO-5b, JO-13a, JO-13b possess potent anti-metastasis ability.
PartII.
Fluorescent labeling has the advantage of high sensitivity and good selectivity for the use in a wide range of applications. In recent years, novel molecular imaging agents were developed for the use of clinical translation through early lesion detection, molecular targeted therapy, therapeutic monitoring, and the development of new anti-cancer drugs. This action significantly improves diagnosis and therapy in patients with breast cancer metastasis. In this thesis, the main structure of our compounds is benzoxazinone. We modified its functional group to explore the relationship between structure and fluorescent quantum yield of molecular probes. Through analysis of the optical property, we found that Jo-35 has the highest quantum yield (Φ = 0.39) compared to that of others. Intramolecular hydrogen bond was confirmed in the skeleton between oxygen atom and amino group of the benzene ring. Molecular probes drop the fluorescent property if the intramolecular hydrogen bond is absent due to replacement of the amino group by other atom and/or moiety.
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author2 |
Wen-Shan Li |
author_facet |
Wen-Shan Li Ming-Xin Liu 劉明鑫 |
author |
Ming-Xin Liu 劉明鑫 |
spellingShingle |
Ming-Xin Liu 劉明鑫 Synthesis and biology of lithocholic acid C4 fluorine-containing sialyltransferase inhitors and benzoxazinone-related fluorescent probes. |
author_sort |
Ming-Xin Liu |
title |
Synthesis and biology of lithocholic acid C4 fluorine-containing sialyltransferase inhitors and benzoxazinone-related fluorescent probes. |
title_short |
Synthesis and biology of lithocholic acid C4 fluorine-containing sialyltransferase inhitors and benzoxazinone-related fluorescent probes. |
title_full |
Synthesis and biology of lithocholic acid C4 fluorine-containing sialyltransferase inhitors and benzoxazinone-related fluorescent probes. |
title_fullStr |
Synthesis and biology of lithocholic acid C4 fluorine-containing sialyltransferase inhitors and benzoxazinone-related fluorescent probes. |
title_full_unstemmed |
Synthesis and biology of lithocholic acid C4 fluorine-containing sialyltransferase inhitors and benzoxazinone-related fluorescent probes. |
title_sort |
synthesis and biology of lithocholic acid c4 fluorine-containing sialyltransferase inhitors and benzoxazinone-related fluorescent probes. |
publishDate |
2015 |
url |
http://ndltd.ncl.edu.tw/handle/6ua4tv |
work_keys_str_mv |
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