Preliminary Structure-Activity Relationship on Theonellasterol, a New Chemotype of FXR Antagonist, from the Marine Sponge Theonella swinhoei

@article{Sepe2012PreliminarySR,
  title={Preliminary Structure-Activity Relationship on Theonellasterol, a New Chemotype of FXR Antagonist, from the Marine Sponge Theonella swinhoei},
  author={Valentina Sepe and Raffaella Ummarino and Maria Valeria D'Auria and Orazio Taglialatela-Scafati and Simona De Marino and Claudio D’Amore and Barbara Renga and Maria Giovanna Chini and Giuseppe Bifulco and Yoichi Nakao and Nobuhiro Fusetani and Stefano Fiorucci and Angela Zampella},
  journal={Marine Drugs},
  year={2012},
  volume={10},
  pages={2448 - 2466}
}
Using theonellasterol as a novel FXR antagonist hit, we prepared a series of semi-synthetic derivatives in order to gain insight into the structural requirements for exhibiting antagonistic activity. These derivatives are characterized by modification at the exocyclic carbon-carbon double bond at C-4 and at the hydroxyl group at C-3 and were prepared from theonellasterol using simple reactions. Pharmacological investigation showed that the introduction of a hydroxyl group at C-4 as well as the… Expand
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