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.
Publication types
-
Research Support, Non-U.S. Gov't
MeSH terms
-
Administration, Oral
-
Animals
-
Antineoplastic Agents / chemical synthesis*
-
Antineoplastic Agents / chemistry
-
Antineoplastic Agents / pharmacokinetics
-
Cell Line, Tumor
-
Drug Screening Assays, Antitumor
-
HSP90 Heat-Shock Proteins / antagonists & inhibitors*
-
HSP90 Heat-Shock Proteins / metabolism
-
Humans
-
Macrolides / chemistry
-
Mice
-
Mice, Inbred ICR
-
Prodrugs / chemical synthesis*
-
Prodrugs / chemistry
-
Prodrugs / pharmacokinetics
-
Xenograft Model Antitumor Assays
Substances
-
Antineoplastic Agents
-
HSP90 Heat-Shock Proteins
-
Macrolides
-
Prodrugs
-
monorden