| Literature DB >> 26432755 |
Rémi Safi1,2, Fréderic Rodriguez2, Georges Hilal3, Mona Diab-Assaf1, Youssef Diab1, Marwan El-Sabban4, Fadia Najjar1, Evelyne Delfourne2.
Abstract
The natural product ferutinin was shown to act as an agonist to estrogen receptor ERα and agonist/antagonist to ERβ 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 μM. 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 ERα protein while ferutinin acts as an agonist.Entities:
Keywords: Ferula hermonis; antitumor agents; breast cancer; estrogen receptors; ferutinin; jaeschkenadiol; molecular docking
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Year: 2015 PMID： 26432755 DOI： 10.1111/cbdd.12670
Source DB: PubMed Journal: Chem Biol Drug Des ISSN： 1747-0277 Impact factor: 2.817