Genistein衍生物之合成及抗癌活性評估

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题名:	Genistein衍生物之合成及抗癌活性評估 Synthesis and Anticancer Bioevaluation of Genistein Derivatives
作者:	林佳民;Chia-Min Lin
贡献者:	藥學院藥物化學研究所碩士班
关键词:	genistein;大豆異黃酮;azaisoflavone;genistein;isoflavone;azaisoflavone
日期:	2010
上传时间:	2010-09-29 14:10:24 (UTC+8)
摘要:	近年來的研究指出，genistein對肝癌、卵巢癌等有不錯的抑制效果。著者合成出一系列的genistein類衍生物，對A549的活性表現可達到IC50 : 26 μM且對JJ012的活性表現也可達到IC50 : 7.53 μM，以genistein作為先導化合物，利用其生物等價異構物 (bioisosterism) 將其pyran以pyridine取代，合成出azaisoflavone再與抗癌生物活性之相關性做探討。初步的實驗結果顯示出，對於肺癌的生物活性可達到IC50 : 8.9 M，且對SW1353的IC50更可達到5.8 μM，綜合以上結果顯示此系列化合物具有抑制軟骨癌細胞及肺癌細胞的潛力。 Recent studies have been indicated that genistein has a great inhibitory effect on liver, ovarian cancer and so on. A series of genistein derivatives was synthesized, which possessed the activity against lung A549 cell line and chondrosarcoma JJ012 cell line with an IC50 value of 26 μM and 7.53 μM, respectively. Follow genistein as lead compound, a series of azaisoflavone was synthesized by bioisosterism and subjected to structure- activity relationship (SAR) study of anticancer activity. The primary results was shown that azaisoflavones demonstrated good activity against lung A549 cell line and chondrosarcoma SW1353 cell line with an IC50 value of 8.9 μM and 5.8 μM, respectively. In this study, we described the SAR study of isoflavone and azaisoflavone and illustrated the activity of genistein derivatives against chondrosarcoma and lung cancer.
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