In vitro hepatic metabolism of 3-amino-6-(3-aminopropyl)-5,6-dihydro-5, 11-dioxo-11H-indeno1,2-c isoquinoline dihydrochloride, a promising lead for cancer chemoprevention

摘要

1. Human liver microsomes formed 1 metabolite of AM6-36, and human liver hepatocytes formed 4 AMS-36 metabolites which were characterized by accurate mass measurement, MS-MS and identified by comparison to synthetic standards. 2. Phase Il amidation was observed but not glucuronidation or suflation. Phase I oxidation reactions were also observed. 3. The metabolic stability of AMS-36 during incubation with human liver microsomes was 3-fold greater than that of the reference compound propranolol.