2-Amino and 2’-Aminocombretastatins Derivatives as Potent Antimitotic Agents
碩士 === 臺北醫學大學 === 藥學系 === 94 === A novel series of 2-amino and 2’-aminocombretastatins derivatives was synthesized and evaluated for antitumor activity. Several compounds had excellent antiproliferative activity as inhibitors of tubulin polymerization. Compound 1, 11, and 12 with IC50 of 1.6, 1...
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ndltd-TW-094TMC005510202015-10-13T10:38:06Z http://ndltd.ncl.edu.tw/handle/56495780464339932541 2-Amino and 2’-Aminocombretastatins Derivatives as Potent Antimitotic Agents 2-胺基與2’-胺基Combretastatins衍生物做為強效抗有絲分裂劑 Yang Ming Fang 楊明芳 碩士 臺北醫學大學 藥學系 94 A novel series of 2-amino and 2’-aminocombretastatins derivatives was synthesized and evaluated for antitumor activity. Several compounds had excellent antiproliferative activity as inhibitors of tubulin polymerization. Compound 1, 11, and 12 with IC50 of 1.6, 1.7, and 1.8 M, respectively, exhibited more potent inhibition of tubulin polymerization than colchicine and approximately as active as CA4. They also displayed antiproliferative activity with an IC50 values ranging from 11 to 44 nM in a variety of human cancer cell lines from different organs. SAR information indicates that the amine substituent at 2-position of ring A or ring B in combretastatin moiety plays an important role in the activity of this series of compounds. Liou Jing Ping 劉景平 2006 學位論文 ; thesis 113 zh-TW |
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碩士 === 臺北醫學大學 === 藥學系 === 94 === A novel series of 2-amino and 2’-aminocombretastatins derivatives was synthesized and evaluated for antitumor activity. Several compounds had excellent antiproliferative activity as inhibitors of tubulin polymerization.
Compound 1, 11, and 12 with IC50 of 1.6, 1.7, and 1.8 M, respectively, exhibited more potent inhibition of tubulin polymerization than colchicine and approximately as active as CA4. They also displayed antiproliferative activity with an IC50 values ranging from 11 to 44 nM in a variety of human cancer cell lines from different organs.
SAR information indicates that the amine substituent at 2-position of ring A or ring B in combretastatin moiety plays an important role in the activity of
this series of compounds.
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author2 |
Liou Jing Ping |
author_facet |
Liou Jing Ping Yang Ming Fang 楊明芳 |
author |
Yang Ming Fang 楊明芳 |
spellingShingle |
Yang Ming Fang 楊明芳 2-Amino and 2’-Aminocombretastatins Derivatives as Potent Antimitotic Agents |
author_sort |
Yang Ming Fang |
title |
2-Amino and 2’-Aminocombretastatins Derivatives as Potent Antimitotic Agents |
title_short |
2-Amino and 2’-Aminocombretastatins Derivatives as Potent Antimitotic Agents |
title_full |
2-Amino and 2’-Aminocombretastatins Derivatives as Potent Antimitotic Agents |
title_fullStr |
2-Amino and 2’-Aminocombretastatins Derivatives as Potent Antimitotic Agents |
title_full_unstemmed |
2-Amino and 2’-Aminocombretastatins Derivatives as Potent Antimitotic Agents |
title_sort |
2-amino and 2’-aminocombretastatins derivatives as potent antimitotic agents |
publishDate |
2006 |
url |
http://ndltd.ncl.edu.tw/handle/56495780464339932541 |
work_keys_str_mv |
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