Discovery of Novel RAD 51 and NF-kB Inhibitors : IBR2 Analogues and Aminofuran fused Benzimidazole and Synthesis of Phosphonyl Pyrazole fused Benzimidazole

碩士 === 國立交通大學 === 應用化學系碩博士班 === 100 === In this thesis, we used multicomponent reactions for synthesis of different main architecture of small organic molecules and did the biological screening for anticancer activity, in order to identify the high inhibition of drug leads. This thesis can be divide...

Full description

Bibliographic Details
Main Author: 洪懿慈
Other Authors: 孫仲銘
Format: Others
Language:zh-TW
Published: 2012
Online Access:http://ndltd.ncl.edu.tw/handle/9dfyeg
id ndltd-TW-100NCTU5500082
record_format oai_dc
spelling ndltd-TW-100NCTU55000822019-05-15T20:52:15Z http://ndltd.ncl.edu.tw/handle/9dfyeg Discovery of Novel RAD 51 and NF-kB Inhibitors : IBR2 Analogues and Aminofuran fused Benzimidazole and Synthesis of Phosphonyl Pyrazole fused Benzimidazole 研發新型RAD 51 與 NF-kB抑制劑:IBR2衍生物以及氨基呋喃鍵結苯并咪唑與合成磷酰吡唑鍵結苯并咪唑 洪懿慈 碩士 國立交通大學 應用化學系碩博士班 100 In this thesis, we used multicomponent reactions for synthesis of different main architecture of small organic molecules and did the biological screening for anticancer activity, in order to identify the high inhibition of drug leads. This thesis can be divided into three parts: The first part reported the improvement of the synthetic approach for the assembling of IBR2 analogues. The original two steps synthetic route was improved to one pot tandem reaction and the reaction time was reduced to 30 minutes from 20 hours. Based on this efficient synthetic approach, a series of IBR2 derivatives were prepared and these IBR2 analogues were subjected to biological screening. The second part informed that the used of 2-cyanomethylbenzimidazole and 2-bromoacetophenone for cyclization reaction to synthesis the molecular library which conformation has the furan structure as well as studied the structure-activity relationship. The third part used 2-cyanomethylbenzimidazole as a starting material through condensation reaction and cyclization reaction with aldehyde and Bestmann-Ohira reagent for synthesis the molecular library which conformation has the pyrazole structure. 孫仲銘 2012 學位論文 ; thesis 60 zh-TW
collection NDLTD
language zh-TW
format Others
sources NDLTD
description 碩士 === 國立交通大學 === 應用化學系碩博士班 === 100 === In this thesis, we used multicomponent reactions for synthesis of different main architecture of small organic molecules and did the biological screening for anticancer activity, in order to identify the high inhibition of drug leads. This thesis can be divided into three parts: The first part reported the improvement of the synthetic approach for the assembling of IBR2 analogues. The original two steps synthetic route was improved to one pot tandem reaction and the reaction time was reduced to 30 minutes from 20 hours. Based on this efficient synthetic approach, a series of IBR2 derivatives were prepared and these IBR2 analogues were subjected to biological screening. The second part informed that the used of 2-cyanomethylbenzimidazole and 2-bromoacetophenone for cyclization reaction to synthesis the molecular library which conformation has the furan structure as well as studied the structure-activity relationship. The third part used 2-cyanomethylbenzimidazole as a starting material through condensation reaction and cyclization reaction with aldehyde and Bestmann-Ohira reagent for synthesis the molecular library which conformation has the pyrazole structure.
author2 孫仲銘
author_facet 孫仲銘
洪懿慈
author 洪懿慈
spellingShingle 洪懿慈
Discovery of Novel RAD 51 and NF-kB Inhibitors : IBR2 Analogues and Aminofuran fused Benzimidazole and Synthesis of Phosphonyl Pyrazole fused Benzimidazole
author_sort 洪懿慈
title Discovery of Novel RAD 51 and NF-kB Inhibitors : IBR2 Analogues and Aminofuran fused Benzimidazole and Synthesis of Phosphonyl Pyrazole fused Benzimidazole
title_short Discovery of Novel RAD 51 and NF-kB Inhibitors : IBR2 Analogues and Aminofuran fused Benzimidazole and Synthesis of Phosphonyl Pyrazole fused Benzimidazole
title_full Discovery of Novel RAD 51 and NF-kB Inhibitors : IBR2 Analogues and Aminofuran fused Benzimidazole and Synthesis of Phosphonyl Pyrazole fused Benzimidazole
title_fullStr Discovery of Novel RAD 51 and NF-kB Inhibitors : IBR2 Analogues and Aminofuran fused Benzimidazole and Synthesis of Phosphonyl Pyrazole fused Benzimidazole
title_full_unstemmed Discovery of Novel RAD 51 and NF-kB Inhibitors : IBR2 Analogues and Aminofuran fused Benzimidazole and Synthesis of Phosphonyl Pyrazole fused Benzimidazole
title_sort discovery of novel rad 51 and nf-kb inhibitors : ibr2 analogues and aminofuran fused benzimidazole and synthesis of phosphonyl pyrazole fused benzimidazole
publishDate 2012
url http://ndltd.ncl.edu.tw/handle/9dfyeg
work_keys_str_mv AT hóngyìcí discoveryofnovelrad51andnfkbinhibitorsibr2analoguesandaminofuranfusedbenzimidazoleandsynthesisofphosphonylpyrazolefusedbenzimidazole
AT hóngyìcí yánfāxīnxíngrad51yǔnfkbyìzhìjìibr2yǎnshēngwùyǐjíānjīfūnánjiànjiéběnbìngmīzuòyǔhéchénglínxiānbǐzuòjiànjiéběnbìngmīzuò
_version_ 1719105978937376768