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- Title
Hemisynthesis, Antitumoral Effect, and Molecular Docking Studies of Ferutinin and Its Analogues.
- Authors
Safi, Rémi; Rodriguez, Fréderic; Hilal, Georges; Diab ‐ Assaf, Mona; Diab, Youssef; El ‐ Sabban, Marwan; Najjar, Fadia; Delfourne, Evelyne
- Abstract
The natural product ferutinin was shown to act as an agonist to estrogen receptor ER α and agonist/antagonist to ER β featuring a weak antiproliferative activity toward breast cancer cells. To enhance this activity, ferutinin analogues were synthesized by esterification of jaeschkenadiol with different acids. These compounds were assayed for their in vitro antiproliferative activity against estrogen-dependent ( MCF-7) and estrogen-independent ( MDA- MB-231) breast cancer cell lines. Among the compounds, 3c' exhibited a potent inhibitory selective activity against MCF-7 with IC50 value of 1 μ m. Docking simulation of 3c' in the ligand binding domain of the ERs indicated a potential antagonism interaction with both ER subtypes. Functional assay showed that 3c' binds as an antagonist to ER α protein while ferutinin acts as an agonist.
- Subjects
ANTINEOPLASTIC agents; MOLECULAR docking; ESTROGEN receptors; ESTERIFICATION; CANCER cells; LIGAND binding (Biochemistry)
- Publication
Chemical Biology & Drug Design, 2016, Vol 87, Issue 3, p382
- ISSN
1747-0277
- Publication type
Article
- DOI
10.1111/cbdd.12670