LXR ANTAGONISTS WITH A 5-SUBSTITUTED PHENANTHRIDIN-6-ONE SKELETON: SYNTHESIS AND LXR TRANSREPRESSION ACTIVITIES OF CONFORMATIONALLY RESTRICTED CARBA-T0901317 ANALOGS

摘要

Conformationally restricted heterocyclic analogs of carba-T0901317, a liver X receptor (LXR) antagonist, were prepared via the palladium catalized cyclization reaction as a key step. In vitro transactivation assay revealed that the structural modification altered the nature of the activity from LXR-agonistic to LXR-antagonistic.