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...
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| Format: | Others |
| Language: | zh-TW |
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2012
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| Online Access: | http://ndltd.ncl.edu.tw/handle/9dfyeg |
| Summary: | 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.
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