Radi Smaail, Tighadouini Said, Feron Olivier, Riant Olivier, Bouakka Mohammed, Benabbes Redouane, Mabkhot Yahia N
Department of Chemistry, Faculty of Sciences, University Mohamed I, Oujda-60000, Morocco.
Angiogenesis and Cancer Research Lab, Pole of Pharmacology and Therapeutics-FATH5349, Institute of Experimental and Clinical Research, Université catholique de Louvain (UCL), Brussels 1200, Belgium.
Molecules. 2015 Nov 10;20(11):20186-94. doi: 10.3390/molecules201119684.
Recently, a new generation of highly promising inhibitors bearing β-keto-enol functionality has emerged. Reported herein is the first synthesis and use of novel designed drugs based on the β-keto-enol group embedded with heterocyclic moieties such as pyrazole, pyridine, and furan, prepared in a one-step procedure by mixed Claisen condensation. All the newly synthesized compounds were characterized by FT-IR, ¹H-NMR, (13)C-NMR, ESI/LC-MS, elemental analysis, and evaluated for their in vitro antiproliferative activity against breast cancer (MDA-MB241) human cell lines and fungal strains (Fusarium oxysporum f.sp albedinis FAO). Three of the synthesized compounds showed potent activity against fungal strains with IC50 values in the range of 0.055-0.092 µM. The results revealed that these compounds showed better IC50 values while compared with positive controls.
最近,出现了新一代具有高度前景的带有β-酮-烯醇官能团的抑制剂。本文报道了基于嵌入吡唑、吡啶和呋喃等杂环部分的β-酮-烯醇基团的新型设计药物的首次合成及应用,该药物通过混合克莱森缩合一步法制备。所有新合成的化合物均通过傅里叶变换红外光谱(FT-IR)、核磁共振氢谱(¹H-NMR)、核磁共振碳谱((13)C-NMR)、电喷雾电离/液相色谱-质谱联用(ESI/LC-MS)、元素分析进行表征,并评估了它们对乳腺癌(MDA-MB241)人类细胞系和真菌菌株(尖孢镰刀菌古巴专化型FAO)的体外抗增殖活性。其中三种合成化合物对真菌菌株显示出强效活性,IC50值在0.055 - 0.092 µM范围内。结果表明,与阳性对照相比,这些化合物显示出更好的IC50值。