Synthesis and Biological Evaluation of Indolyl-Pyridinyl-Propenones Having Either Methuosis or Microtubule Disruption Activity

CJ Trabbic, JH Overmeyer, EM Alexander…

Index: Trabbic, Christopher J.; Dietsch, Heather M.; Alexander, Evan M.; Nagy, Peter I.; Robinson, Michael W.; Overmeyer, Jean H.; Maltese, William A.; Erhardt, Paul W. ACS Medicinal Chemistry Letters, 2014 , vol. 5, # 1 p. 73 - 77

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Citation Number: 7

Abstract

Methuosis is a form of nonapoptotic cell death characterized by an accumulation of macropinosome-derived vacuoles with eventual loss of membrane integrity. Small molecules inducing methuosis could offer significant advantages compared to more traditional anticancer drug therapies that typically rely on apoptosis. Herein we further define the effects of chemical substitutions at the 2-and 5-indolyl positions on our lead compound ...