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Synthesis, Biological Evaluation, and Molecular Docking Studies of Xanthone Sulfonamides as ACAT Inhibitors

Xiang Li, Yan Zou, Qingjie Zhao, Yan Yang, Maocheng Wu, Ting Huang, Honggang Hu, Qiuye Wu

Chem Biol Drug Des. 2015 Mar;85(3):394-403.

PMID: 25146964

Abstract:

Three series of xanthone sulfonamides were synthesized, and their inhibitory activities against acyl-CoA: cholesterol acyltransferase (ACAT) were evaluated. Results showed that most of the title compounds exhibited strong inhibitory activity against ACAT, of which compounds 1c, 1e, 1f, 2d, 2e, and 3d were proved to be more active than the positive control Sandoz 58-035. Computational docking experiments indicated that the interaction between inhibitors and ACAT contained the H-bond interaction, the hydrophobic interaction, and the narrow hydrophobic cleft.

Chemicals Related in the Paper:

Catalog Number Product Name Structure CAS Number Price
AP78934835 Sandoz 58-035 Sandoz 58-035 78934-83-5 Price
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