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Publication 58  

  1. Synthesis of pochoxime prodrugs as potent HSP90 inhibitors
    C. Wang, S. Barluenga, G. K. Koripelly, J.-G. Fontaine, R. Chen, J.-C. Yu, X. Shen, J. C. Chabala, J. V. Heck, A. Rubenstein, N. Winssinger
    Bioorg. Med. Chem. Lett. 2009, 19, 3836-3840

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.

DOI : 10.1016/j.bmcl.2009.04.030 

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