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Preliminary structure-activity relationship on theonellasterol, a new chemotype of FXR antagonist, from the marine sponge Theonella swinhoei.

Abstract：

: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 oxidation at C-3 with or without concomitant modification at the exomethylene functionality preserve the ability of theonellasterol to inhibit FXR transactivation caused by CDCA. Docking analysis showed that the placement of these molecules in the FXR-LBD is well stabilized when on ring A functional groups, able to form hydrogen bonds and π interactions, are present.

journal_name

Mar Drugs

journal_title

Marine drugs

authors

Sepe V,Ummarino R,D'Auria MV,Taglialatela-Scafati O,Marino SD,D'Amore C,Renga B,Chini MG,Bifulco G,Nakao Y,Fusetani N,Fiorucci S,Zampella A

doi

10.3390/md10112448

subject

Has Abstract

pub_date

2012-11-05 00:00:00

pages

2448-66

issue

11

issn

1660-3397

pii

md10112448

journal_volume

10

pub_type

杂志文章

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