Synthesis of AHPN Derivatives and Their Combining Activities with RARγ
- Author:
Bin-Shan ZHANG
1
Author Information
- Publication Type:Journal Article
- Keywords: AHPN; RARγ; Synthesis; Targeted binding
- From: Chinese Pharmaceutical Journal 2018;53(4):249-257
- CountryChina
- Language:Chinese
- Abstract: OBJECTIVE: To study the synthesis and activities of AHPN derivatives. METHODS: Starting from p-bromophenol and 1-adamantanol, a series of AHPN derivatives were synthesized by substitution reaction, condensation reaction, oxidation reaction and reduction reaction. These new compounds were characterized by 1H-NMR, 13CNMR and HR-MS. Biacore technique was used to test the derivatives' combining activities with RARγ. RESULTS: Four compounds, 7c, 6c, 6e, and 6h, exhibited significant combining activities with RARγ compared with AHPN. The introduction of phosphoric acid groups and nitrogen heterocyclic ring increased the activities of these compounds. CONCLUSION: Compounds 7c, 6c, 6e, and 6h show significant combining activities with RARγ, which are worthy of further study.
