Synthesis and Biological Evaluation of Oxime- and Amide-e-containing Coumarin Derivatives

Chia Nan University of Pharmacy & Science Institutional Repository > 藥理學院 > 2011年台俄有機、藥物與生物化學交流暨藥物化學研討會 > Item 310902800/24234

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標題:	Synthesis and Biological Evaluation of Oxime- and Amide-e-containing Coumarin Derivatives
作者:	Ken-Ming Chang (張耿銘) Tai-Chi Wang (王泰吉) I-Li Chen (陳意莉) Cherng-Chyi Tzeng (曾誠齊)
日期:	2011
上傳時間:	2011-06-23 14:57:23 (UTC+8)
摘要:	Recently, we have synthesized certain coumarin a-methylene-y-butyrolactorones for biological evaluations. Some of them were found to possess cardiovascular effects while others have been proved to be potential antiproliferative agents. A numbeier of oxime- and amide bearing quinolin-2(lH)-one derivatives have also been synthesized and demonstrated to possess anti-inflammatory and antiproliferative activities.To explore novel type of biologically active coumarin derivatives, we have synthesized a series of oxime and amide bearing coumarins and evaluated for their biological activities. These compounds were synthesized via alkylation of hydroxyylated coumarin precursors followed by the reaction with NH2OH or NaN3 (Schmidt reaction). The preliminary assays indicated that oxime-containing coumarin derivatives possessed good inhibitory activities on the fMLP-induced inflammation while the amide-conntaiaining coumarin derivatives exhibited potent antiproliferative activities against the growth of NPC-TW01, H661 and Jurkat cell lines. The cell cycle analysis showed that the amide-containing coumarin derivatives rested NPC-TW01 cells at S phase with dose-dependent manner.
關聯:	2011年台俄有機、藥物與生物化學交流暨藥物化學研討會，起迄日：2011/04/06~2011/04/05，地點：溪頭台大實驗林
显示于类别:	[藥理學院] 2011年台俄有機、藥物與生物化學交流暨藥物化學研討會

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