1604818-95-2Relevant academic research and scientific papers
Total synthesis and RXRα-mediated transcription studies of neriifolone B and related compounds
Shen, Qirong,Dai, Yi,Wang, Guanghui,Yao, Fei,Duan, Yinghui,Chen, Haifeng,Zhang, Weige,Zhang, Xiaokun,Yao, Xinsheng
, p. 2671 - 2677 (2014/05/06)
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.
