o-(chloroacetylcarbamoyl)fumagillol and 8-mercaptoquinoline

This paper describes a reversed-phase, high-performance liquid chromatographic (HPLC) method for the isolation, detection, and quantification of TNP-470 (I) and one of its active metabolites, AGM-1883 (II), from plasma. These compounds are initially extracted from plasma with an organic solvent and then separated from one another on a C18 column. Those fractions eluting from the C18 column and containing either I or II are then derivatized through their epoxide moieties with sodium 8-quinolinethiolate (SQT). This derivatization produces fluorescent species that are isolated and quantified by a second reversed-phase HPLC analysis. The assay yields a lower limit of reliable quantification of 2.5 ng/ml and is linear to a concentration at least as high as 160 ng/ml. The inter-assay percent coefficient of variation is less than 18%.

Topics: Acetamides; Antibiotics, Antineoplastic; Chromatography, High Pressure Liquid; Cyclohexanes; Epoxy Compounds; Humans; Magnetic Resonance Spectroscopy; O-(Chloroacetylcarbamoyl)fumagillol; Quinolines; Sensitivity and Specificity; Sesquiterpenes; Spiro Compounds