Evaluating the potential of vacuolar ATPase inhibitors as anticancer agents and multigram synthesis of the potent salicylihalamide analog saliphenylhalamide

…, MG Roth, DA Ferguson, JK De Brabander

Index: Lebreton, Sylvain; Jaunbergs, Janis; Roth, Michael G.; Ferguson, Deborah A.; De Brabander, Jef K. Bioorganic and Medicinal Chemistry Letters, 2008 , vol. 18, # 22 p. 5879 - 5883

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Citation Number: 36

Abstract

The natural product salicylihalamide is a potent inhibitor of the Vacuolar ATPase (V- ATPase), a potential target for antitumor chemotherapy. We generated salicylihalamide- resistant tumor cell lines typified by an overexpansion of lysosomal organelles. We also found that many tumor cell lines upregulate tissue-specific plasmalemmal V-ATPases, and hypothesize that tumors that derive their energy from glycolysis rely on these isoforms to ...