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（Z）-3-（2-氨乙基）-5-（4-乙氧基苯亚甲基）噻唑烷-2,4-二酮的结构修饰，提高了对含有活跃 ERK 信号的黑色素瘤细胞增殖的抑制选择性。

Structural modifications of (Z)-3-(2-aminoethyl)-5-(4-ethoxybenzylidene)thiazolidine-2,4-dione that improve selectivity for inhibiting the proliferation of melanoma cells containing active ERK signaling.

机构信息

Department of Pharmaceutical Sciences, University of Maryland School of Pharmacy, 20 N Pine St., Baltimore, MD 21201, USA.

出版信息

Org Biomol Chem. 2013 Jun 14;11(22):3706-32. doi: 10.1039/c3ob40199e.

DOI:10.1039/c3ob40199e
PMID:23624850
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC3663054/
Abstract

We herein report on the pharmacophore determination of the ERK docking domain inhibitor (Z)-3-(2-aminoethyl)-5-(4-ethoxybenzylidene)thiazolidine-2,4-dione, which has led to the discovery of compounds with greater selectivities for inhibiting the proliferation of melanoma cells containing active ERK signaling.

摘要

我们在此报告 ERK 对接结构域抑制剂（Z）-3-(2-氨乙基）-5-(4-乙氧基苯亚甲基）噻唑烷-2,4-二酮的药效团确定，这导致了发现对含有活性 ERK 信号的黑色素瘤细胞增殖具有更高选择性的化合物。

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ERK inhibition overcomes acquired resistance to MEK inhibitors.ERK 抑制可克服对 MEK 抑制剂的获得性耐药。
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