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

Kwan-Young Jung; Ramin Samadani; Jay Chauhan; Kerrick Nevels; Jeremy L. Yap; Jun Zhang; Shilpa Worlikar; Maryanna E. Lanning; Lijia Chen; Mary Ensey; Sagar Shukla; Rosene Salmo; Geoffrey Heinzl; Caryn Gordon; Troy Dukes; Alexander D. MacKerell, Jr.; Paul Shapiro; Steven Fletcher

doi:10.1039/C3OB40199E

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

Kwan-Young Jung,†^a Ramin Samadani,†^a Jay Chauhan,^a Kerrick Nevels,^a Jeremy L. Yap,^a Jun Zhang,^a Shilpa Worlikar,^a Maryanna E. Lanning,^a Lijia Chen,^a Mary Ensey,^b Sagar Shukla,^a Rosene Salmo,^c Geoffrey Heinzl,^a Caryn Gordon,^d Troy Dukes,^e Alexander D. MacKerell, Jr.,^af Paul Shapiro*^af and Steven Fletcher*^af

Author affiliations

* Corresponding authors

^a Department of Pharmaceutical Sciences, University of Maryland School of Pharmacy, 20 N Pine St., Baltimore, MD 21201, USA
E-mail: sfletche@rx.umaryland.edu, pshapiro@rx.umaryland.edu
Fax: +1 410 706 5017
Tel: +1 410 706 6361

^b Notre Dame of Maryland University, 4701 N Charles Street, Baltimore, MD 21212, USA

^c Indiana University Purdue University Indianapolis, 420 University Boulevard Indianapolis, IN 46202, USA

^d University of Maryland, College Park, MD 20742, USA

^e Antioch Diploma Plus High School, 2555 Harford Road, Baltimore, MD 21218, USA

^f University of Maryland Greenebaum Cancer Center, Baltimore, MD 21201, USA

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.

This article is part of the themed collection: In Celebration of Andrew D. Hamilton’s Career in Chemistry

Organic & Biomolecular Chemistry

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

Article information

Download Citation

Permissions

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

Social activity

Search articles by author

Spotlight

Advertisements