Ontology highlight
ABSTRACT:
SUBMITTER: Blois J
PROVIDER: S-EPMC2663427 | biostudies-literature | 2008 Aug
REPOSITORIES: biostudies-literature
Blois Joseph J Yuan Hushan H Smith Adam A Pacold Michael E ME Weissleder Ralph R Cantley Lewis C LC Josephson Lee L
Journal of medicinal chemistry 20080717 15
When the viridin wortmannin (Wm) is modified by reaction with certain nucleophiles at the C20 position, the compounds obtained exhibit an improved antiproliferative activity even though a covalent reaction between C20 and a lysine in the active site of PI3 kinase is essential to Wm's ability to inhibit this enzyme. Here we show that this improved potency results from an intramolecular attack by the C6 hydroxyl group that slowly converts these inactive prodrugs to the active species Wm over the 4 ...[more]