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

Article scientifique

Anglais

Synthesis of pochoxime prodrugs as potent HSP90 inhibitors

Contributeurs/tricesWang, 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

Publié dansBioorganic & medicinal chemistry letters, vol. 19, no. 14, p. 3836-3840

Date de publication2009

Résumé

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.

Mots-clés

HSP90
Radicicol
Pochoxime
Prodrug

Structure d'affiliation Pas une publication de l'UNIGE

Citation (format ISO)

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)

Identifiants

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

URL commercialhttp://linkinghub.elsevier.com/retrieve/pii/S0960894X0900496X

ISSN du journal0960-894X

466vues

0téléchargements

Création12/12/2012 09:32:00

Première validation12/12/2012 09:32:00

Heure de mise à jour14/03/2023 17:47:52

Changement de statut14/03/2023 17:47:52

Dernière indexation16/01/2024 00:40:31

Archive ouverte UNIGE

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.

Informations techniques