Ontology highlight
ABSTRACT:
SUBMITTER: Ammazzalorso A
PROVIDER: S-EPMC7236056 | biostudies-literature | 2020 May
REPOSITORIES: biostudies-literature
ACS medicinal chemistry letters 20200303 5
An agonist-antagonist switching strategy was performed to discover novel PPARα antagonists. Phenyldiazenyl derivatives of fibrates were developed, bearing sulfonimide or amide functional groups. A second series of compounds was synthesized, replacing the phenyldiazenyl moiety with amide or urea portions. Final compounds were screened by transactivation assay, showing good PPARα antagonism and selectivity at submicromolar concentrations. When tested in cancer cell models expressing PPARα, selecte ...[more]