Synthesis of pochoxime prodrugs as potent HSP90 inhibitors

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

doi:10.1016/j.bmcl.2009.04.030

Scientific article

English

Synthesis of pochoxime prodrugs as potent HSP90 inhibitors

ContributorsWang, 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

Published inBioorganic & medicinal chemistry letters, vol. 19, no. 14, p. 3836-3840

Publication date2009

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.

Keywords

HSP90
Radicicol
Pochoxime
Prodrug

Affiliation entities

Not a UNIGE publication

Citation (ISO format)

WANG, Cuihua et al. Synthesis of pochoxime prodrugs as potent HSP90 inhibitors. In: Bioorganic & medicinal chemistry letters, 2009, vol. 19, n° 14, p. 3836–3840. doi: 10.1016/j.bmcl.2009.04.030

Article (Published version)

Identifiers

PID : unige:24721
DOI : 10.1016/j.bmcl.2009.04.030

Additional URL for this publicationhttp://linkinghub.elsevier.com/retrieve/pii/S0960894X0900496X

Journal ISSN0960-894X

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Synthesis of pochoxime prodrugs as potent HSP90 inhibitors

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.

Technical informations