Amide derivatives of ethacrynic acid: synthesis and evaluation as antagonists of Wnt/beta-catenin signaling and CLL cell survival.
Amide derivatives of ethacrynic acid: synthesis and evaluation as antagonists of Wnt/beta-catenin signaling and CLL cell survival.
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DOI：
10.1016/j.bmcl.2008.12.067
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发表时间：
2009-02-01
影响因子：
2.7
通讯作者：
Cottam HB
中科院分区：
文献类型：
--
作者：
Jin G;Lu D;Yao S;Wu CC;Liu JX;Carson DA;Cottam HB
制备了一系列依他尼酸酰胺，并评价了它们抑制Wnt信号传导和降低CLL细胞存活的能力。几种最有效的衍生物在低微摩尔范围内具有活性。EA的α，β-不饱和碳-碳双键的还原消除了Wnt信号传导的抑制以及CLL存活的降低。初步作用机制研究表明，这些衍生物共价修饰对Wnt/β-连环蛋白信号传导重要的转录因子上存在的巯基。
A series of amides of ethacrynic acid was prepared and evaluated for their ability to inhibit Wnt signaling and decrease the survival of CLL cells. Several of the most potent derivatives were active in the low micromolar range. Reduction of the α,β-unsaturated carbon–carbon double bond of EA abrogated both the inhibition of Wnt signaling as well as the decrease in CLL survival. Preliminary mechanism of action studies suggest that these derivatives covalently modify sulfhydryl groups present on transcription factors important for Wnt/β-catenin signaling.
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影响因子：
64.8
作者：
Rossi, A;Kapahi, P;Santoro, MG
通讯作者：
Santoro, MG
DOI：
10.1073/pnas.0504600102
发表时间：
2005-08-23
影响因子：
11.1
作者：
Teo, JL;Ma, H;Kahn, M
通讯作者：
Kahn, M
DOI：
10.1073/pnas.0509316102
发表时间：
2005-12-20
影响因子：
11.1
作者：
Lu, DS;Cottam, HB;Carson, DA
通讯作者：
Carson, DA
影响因子：
5.7
作者：
Aizawa, S;Ookawa, K;Tsuchida, S
通讯作者：
Tsuchida, S
DOI：
10.1016/j.bbrc.2005.03.242
发表时间：
2005-06-17
影响因子：
3.1
作者：
Park, CH;Hahm, ER;Yang, CH
通讯作者：
Yang, CH