Yncréa Hauts-de-France, Laboratory of Sustainable Chemistry and Health, Health & Environment Department, Team Sustainable Chemistry, Ecole des Hautes Etudes d'Ingénieur (HEI), UCLille, 13 rue de Toul, F-59046 Lille, France.
Yncréa Hauts-de-France, Laboratory of Sustainable Chemistry and Health, Health & Environment Department, Team Sustainable Chemistry, Ecole des Hautes Etudes d'Ingénieur (HEI), UCLille, 13 rue de Toul, F-59046 Lille, France; Univ. Lille, Inserm, CHU Lille, Institut Pasteur de Lille, U1167 - RID-AGE - Facteurs de risque et déterminants moléculaires des maladies liées au vieillissement, F-59000 Lille, France.
Bioorg Med Chem Lett. 2020 Jun 1;30(11):127149. doi: 10.1016/j.bmcl.2020.127149. Epub 2020 Mar 29.
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.
采用超声探头，方便快捷地进行（杂）芳基酮和（杂）芳基醛的克莱森-施密特缩合反应，合成了一系列的查耳酮及其衍生物。与经典的磁力搅拌实验进行了比较，并进行了优化研究，结果表明氢氧化锂是研究缩合反应的最佳碱性催化剂。反应的副产物（β-羟基酮、二酮和环己醇）也被分离出来。所有化合物都在体外评估了它们抑制人法呢基转移酶的能力，法呢基转移酶是一种与癌症和罕见疾病有关的蛋白质，也是 NCI-60 癌细胞系面板的一部分。这些分子对靶蛋白表现出抑制活性，并对不同的细胞系表现出细胞抑制作用，对 MCF7（乳腺癌细胞）具有特别的活性。
