Synthesis of pochoxime prodrugs as potent HSP90 inhibitors

C Wang, S Barluenga, GK Koripelly, JG Fontaine…

Index: Wang, Cuihua; Barluenga, Sofia; Koripelly, Girish K.; Fontaine, Jean-Gonzague; Chen, Ruihong; Yu, Jin-Chen; Shen, Xiaodong; Chabala, John C.; Heck, James V.; Rubenstein, Allan; Winssinger, Nicolas Bioorganic and Medicinal Chemistry Letters, 2009 , vol. 19, # 14 p. 3836 - 3840

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Citation Number: 23

Abstract

Pochoximes are potent inhibitors of heat shock protein 90 (HSP90) based on the radicicol pharmacophores. Herein we present a pharmacokinetics and pharmacodynamics evaluation of this compound series as well as a phosphate prodrug strategy to facilitate formulation and improve oral bioavailability.