【文章名】LXR antagonists with a 5-substituted phenanthridin-6-one skeleton: synthesis and LXR transrepression activities of conformationally restricted carba-T0901317 analogs.
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 prepd. via the palladium catalyzed 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.
