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Discovery of Novel Myc−Max Heterodimer Disruptors with a Three-Dimensional Pharmacophore Model

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journal contribution
posted on 2009-03-12, 00:00 authored by Gabriela Mustata, Ariele Viacava Follis, Dalia I. Hammoudeh, Steven J. Metallo, Huabo Wang, Edward V. Prochownik, John S. Lazo, Ivet Bahar
A three-dimensional pharmacophore model was generated utilizing a set of known inhibitors of c-Myc−Max heterodimer formation. The model successfully identified a set of structurally diverse compounds with potential inhibitory activity against c-Myc. Nine compounds were tested in vitro, and four displayed affinities in the micromolar range and growth inhibitory activity against c-Myc-overexpressing cells. These studies demonstrate the applicability of pharmacophore modeling to the identification of novel and potentially more puissant inhibitors of the c-Myc oncoprotein.