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Article Dans Une Revue Bioorganic and Medicinal Chemistry Letters Année : 2020

Ultrasounds-mediated 10-seconds synthesis of chalcones as potential farnesyltransferase inhibitors

Résumé

A broad range of chalcones and derivatives were easily and rapidly synthesized, following Claisen-Schmidt condensation of (hetero)aryl ketones and (hetero)aryl aldehydes using a ultrasound probe. A comparison was made with classical magnetic stirring experiments, and an optimization study was realized, showing lithium hydroxide to be the best basic catalyst of the studied condensations. By-products of the reactions (β-hydroxy-ketone, diketones, and cyclohexanols) were also isolated. All compounds were evaluated in vitro for their ability to inhibit human farnesyltransferase, a protein implicated in cancer and rare diseases and on the NCI-60 cancer cell lines panel. Molecules showed inhibitory activity on the target protein and cytostatic effect on different cell lines with particular activity against MCF7, breast cancer cells.

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Chimie
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hal-03490383 , version 1 (20-05-2022)

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Germain Homerin, Adrian Sorin Nica, Amaury Farce, Joëlle Dubois, Alina Ghinet. Ultrasounds-mediated 10-seconds synthesis of chalcones as potential farnesyltransferase inhibitors. Bioorganic and Medicinal Chemistry Letters, 2020, 30, pp.127149 -. ⟨10.1016/j.bmcl.2020.127149⟩. ⟨hal-03490383⟩
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