Unexpected tandem ylide annulation reaction for controllable synthesis of 2H-chromenes and 4H-chromenes.

Described herein are compounds that are estrogen receptor modulators. Also described are pharmaceutical compositions and medicaments that include the compounds described herein, as well as methods of using such estrogen receptor modulators, alone and in combination with other compounds, for treating diseases or conditions that are mediated or dependent upon estrogen receptors.

Estrogen receptor modulators and uses thereof

Estrogen signaling: An emanating therapeutic target for breast cancer treatment.

In the search for xenoestrogens within food additives, we have analyzed the Joint FAO-WHO expert committee database, containing 1500 compounds, using an integrated in silico and in vitro approach. This analysis identified 31 potential estrogen receptor α ligands that were reduced to 13 upon applying a stringent filter based on ligand volume and binding mode. Among the 13 potential xenoestrogens, four were already known to exhibit an estrogenic activity, and the other nine were assayed in vitro, determining the binding affinity to the receptor and biological effects. Propyl gallate was found to act as an antagonist, and 4-hexylresorcinol was found to act as a potent transactivator; both ligands were active at nanomolar concentrations, as predicted by the in silico analysis. Some caution should be issued for the use of propyl gallate and 4-hexylresorcinol as food additives.

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Identification of Xenoestrogens in Food Additives by an Integrated in Silico and in Vitro Approach

The consequences of scoring docked ligand conformations using free energy correlations.

Synthesis, pharmacological evaluation, and structure-activity relationships of benzopyran derivatives with potent SERM activity.

2H-1-Benzopyran derivatives, processes for their preparation and use thereof for the preparation of pharmaceutical compositions for the prevention and treatment of postmenopausal pathologies.

Maurizio Civelli

Papers

Synthesis, pharmacological evaluation, and structure-activity relationships of benzopyran derivatives with potent SERM activity.

2H-1-benzopyran derivatives processes for their preparation and pharmaceutical compositions thereof