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

被引：27

作者：

Jung, Kwan-Young ^{[1
]}

Samadani, Ramin ^{[1
]}

Chauhan, Jay ^{[1
]}

Nevels, Kerrick ^{[1
]}

Yap, Jeremy L. ^{[1
]}

Zhang, Jun ^{[1
]}

Worlikar, Shilpa ^{[1
]}

Lanning, Maryanna E. ^{[1
]}

Chen, Lijia ^{[1
]}

Ensey, Mary ^{[2
]}

Shukla, Sagar ^{[1
]}

Salmo, Rosene ^{[3
]}

Heinzl, Geoffrey ^{[1
]}

Gordon, Caryn ^{[4
]}

Dukes, Troy ^{[5
]}

MacKerell, Alexander D., Jr. ^{[1
,6
]}

Shapiro, Paul ^{[1
,6
]}

Fletcher, Steven ^{[1
,6
]}

机构：

[1] Univ Maryland, Sch Pharm, Dept Pharmaceut Sci, Baltimore, MD 21201 USA

[2] Notre Dame Maryland Univ, Baltimore, MD 21212 USA

[3] Indiana Univ Purdue Univ, Indianapolis, IN 46202 USA

[4] Univ Maryland, College Pk, MD 20742 USA

[5] Antioch Diploma Plus High Sch, Baltimore, MD 21218 USA

[6] Univ Maryland, Greenebaum Canc Ctr, Baltimore, MD 21201 USA

来源：

ORGANIC & BIOMOLECULAR CHEMISTRY | 2013年 / 11卷 / 22期

基金：

美国国家卫生研究院;

关键词：

TYROSINE KINASE INHIBITORS; RAF/MEK/ERK PATHWAY; MAP KINASES; RESISTANCE; CANCER; BRAF; MUTATIONS; DISCOVERY; DOMAIN; GENE;

D O I：

10.1039/c3ob40199e

中图分类号：

O62 [有机化学];

学科分类号：

070303 ; 081704 ;

摘要：

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.

引用

页码：3706 / 3732

页数：27

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