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Updated: May 1, 2026

Reverse Yeast Two-hybrid System to Identify Mammalian Nuclear Receptor Residues that Interact with Ligands and/or Antagonists
Published on: November 15, 2013
Total synthesis and RXRα-mediated transcription studies of neriifolone B and related compounds
Qirong Shen1, Yi Dai2, Guanghui Wang3
1Key Laboratory of Structure-Based Drug Design & Discovery, Ministry of Education, Shenyang Pharmaceutical University, Shenyang 110016, People's Republic of China.
Abstract:
Neriifolone B (1), a natural product containing a novel 4',4'-dimethyl-4',5'-dihydropyran-6-one[2',3':3,4]xanthone skeleton, was found to be a potent inhibitor of transcription mediated by retinoid X receptor α (RXRα). The first total synthesis of neriifolone B (1) was achieved in 14 steps with an overall yield of 7.1%. A Claisen rearrangement was employed as the key step in the sequence. The activity of six natural xanthones and eight compounds related to neriifolone B (1) against RXRα-mediated transcription was evaluated. Two neriifolone B analogs, 17 and 11″, were potent inhibitors of RXRα transcriptional activity. Preliminary structure-activity relationship studies are discussed briefly.
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