title: Synthesis of pochoxime prodrugs as potent HSP90 inhibitors.
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.
authors.affiliation: Institute de Science et d'Ingénierie Supramoleculaires, Université de Strasbourg, Strasbourg, France.
authors.forename: Cuihua
authors.initials: C
authors.lastname: Wang
authors.forename: Sofia
authors.initials: S
authors.lastname: Barluenga
authors.forename: Girish K
authors.initials: GK
authors.lastname: Koripelly
authors.forename: Jean-Gonzague
authors.initials: JG
authors.lastname: Fontaine
authors.forename: Ruihong
authors.initials: R
authors.lastname: Chen
authors.forename: Jin-Chen
authors.initials: JC
authors.lastname: Yu
authors.forename: Xiaodong
authors.initials: X
authors.lastname: Shen
authors.forename: John C
authors.initials: JC
authors.lastname: Chabala
authors.forename: James V
authors.initials: JV
authors.lastname: Heck
authors.forename: Allan
authors.initials: A
authors.lastname: Rubenstein
authors.forename: Nicolas
authors.initials: N
authors.lastname: Winssinger
mesh_terms: D000284:Administration, Oral; D000818:Animals; D000970:Antineoplastic Agents / Q000138:chemical synthesis* / Q000737:chemistry / Q000493:pharmacokinetics; D045744:Cell Line, Tumor; D004354:Drug Screening Assays, Antitumor; D018841:HSP90 Heat-Shock Proteins / Q000037:antagonists & inhibitors* / Q000378:metabolism; D006801:Humans; D018942:Macrolides / Q000737:chemistry; D051379:Mice; D008813:Mice, Inbred ICR; D011355:Prodrugs / Q000138:chemical synthesis* / Q000737:chemistry / Q000493:pharmacokinetics; D023041:Xenograft Model Antitumor Assays
chemical_list: D000970:Antineoplastic Agents; D018841:HSP90 Heat-Shock Proteins; D018942:Macrolides; D011355:Prodrugs; C035359:monorden