Aminostyrylbenzofuran derivatives as potent inhibitors for Aβ fibril formation
Aminostyrylbenzofuran derivatives as potent inhibitors for Aβ fibril formation
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DOI：
10.1016/j.bmcl.2008.08.111
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发表时间：
2008-10-15
影响因子：
2.7
通讯作者：
Yoo, Kyung Ho
中科院分区：
文献类型：
--
作者：
Byun, Ji Hun;Kim, HyeYun;Yoo, Kyung Ho
报道了一系列新的氨基苯基苯并呋喃衍生物1a-w的合成及其对Aβ纤维形成的抑制活性。用硫代黄素T(THT)测定了所有化合物的活性，结果表明化合物对Aβ原纤维的形成具有较强的抑制活性。其中，化合物1I和1Q的抑制活性(IC(50)分别为0.07和0.08µM)明显优于姜黄素(IC(50)=0.80µM)和IMSB(IC(50)=8.00µM)作为参比化合物。这两个化合物都被选为有希望进行进一步生物学评价的候选化合物。(C)2008爱思唯尔有限公司。保留所有权利。
The synthesis of a novel series of aminostyrylbenzofuran derivatives 1a-w and their inhibitory activities for A beta fibril formation were described. All the synthesized compounds were evaluated by thioflavin T (ThT) assay and displayed potent inhibitory activities for A beta fibril formation. Among them, compounds 1i and 1q exhibited excellent inhibitory activities (IC(50) = 0.07 and 0.08 mu M, respectively) than those of Curcumin (IC(50) = 0.80 mu M) and IMSB (IC(50) = 8.00 mu M) as reference compounds. Both compounds were selected as promising candidates for further biological evaluation. (C) 2008 Elsevier Ltd. All rights reserved.