Issue 22, 2013

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

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.

Graphical abstract: 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

Article information

Article type
Paper
Submitted
30 jan 2013
Accepted
09 apr 2013
First published
09 apr 2013

Org. Biomol. Chem., 2013,11, 3706-3732

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

K. Jung, R. Samadani, J. Chauhan, K. Nevels, J. L. Yap, J. Zhang, S. Worlikar, M. E. Lanning, L. Chen, M. Ensey, S. Shukla, R. Salmo, G. Heinzl, C. Gordon, T. Dukes, A. D. MacKerell, Jr., P. Shapiro and S. Fletcher, Org. Biomol. Chem., 2013, 11, 3706 DOI: 10.1039/C3OB40199E

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