Selenolopyrazole 類緣物之合成與生物活性

中國醫藥大學機構典藏 China Medical University Repository, Taiwan > 藥學院 > 藥物化學研究所 > 研究計畫 > Item 310903500/13353

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题名:	Selenolopyrazole 類緣物之合成與生物活性
作者:	郭盛助(Kuo,Sheng-Chu);黃麗嬌(Huang,Li-Jiau)
贡献者:	藥學院藥物化學研究所
关键词:	抗癌;腎癌;肺癌;Anti-cancer;Renal cancer;Lung cancer;Selenopyrazole;YC-1
日期:	2007-07-31
上传时间:	2009-09-01 16:20:03 (UTC+8)
摘要:	合成了一系列的YC-1之 selenopyrazde類緣物及其相關化合物來並測試其cytotoxicity，結果發現1-benzyl-3-(2- hydroxymethyl-5-furyl)seleno[3,2-c]pyrazole(I-8)最具潛力，進而以NCI60種 humancancercellline測試其cytotoxicity。再將測試結果加以分析，製作dose-responsecurves，並計算其 GI50、TGI及IC50，而得到相對應的meangraph(Fingerprint)。從fingerprint得知化合物I-8對大多數 cancercellline都具有活性，logGI50之meangraphmidpoint(MG-MID)為-4.68，而活性最高者為對NCI- H226(logGI50為-6.50)及A-498(logGI50為-6.79)，比MG-MID強100倍。基於上述的發現，我們確認化合物I-8 是具有開發潛能的抗肺癌及抗腎癌候選物質。 A series selenopyrazde analogs of YC-1 and related compounds were synthesized and evaluated for their cytotoxicity. Among those tested compounds 1-benzyl-3-(2-hydroxymethyl-5-furyl)seleno[ 3,2-c]pyrazole (I-8) was the most promising agent which was evaluated for cytotoxicity activity against the NCI human cancer cell line panel. The results were analyzed computationally and presented as dose-response curves, at five different concentration between 10-4 and 10-6 M. GI50、TGI and IC50 values were calculated and the corresponding mean graph was obtained. The results showed than compound I-8 was active against most tested cancer cell lines with mean growth midpoint (MG-MID) for log GI50 equal to -4.68. The highest potency was found against NCI-H226 (log GI50, -6.50) and A-498 (log GI50, -6.79). Based on the above finding, compound I-8 was idenfified in this study as a promising anti-lung cancer and anti-renal cancer drug candidate.
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