Synthesis of Novel β-Keto-Enol Derivatives Tethered Pyrazole, Pyridine and Furan as New Potential Antifungal and Anti-Breast Cancer Agents

被引:36
|
作者
Radi, Smaail [1 ]
Tighadouini, Said [1 ]
Feron, Olivier [2 ]
Riant, Olivier [3 ]
Bouakka, Mohammed [4 ]
Benabbes, Redouane [4 ]
Mabkhot, Yahia N. [5 ]
机构
[1] Univ Mohamed I, Fac Sci, Dept Chem, Oujda 60000, Morocco
[2] Catholic Univ Louvain, Angiogenesis & Canc Res Lab, Pole Pharmacol & Therapeutics FATH5349, Inst Expt & Clin Res, B-1200 Brussels, Belgium
[3] Catholic Univ Louvain, Mol Solids & React MOST, Inst Condensed Mater & Nanosci IMCN, B-1348 Louvain, Belgium
[4] Univ Mohamed I, Fac Sci, Dept Biol, Oujda 60000, Morocco
[5] King Saud Univ, Dept Chem, Fac Sci, Riyadh 11451, Saudi Arabia
来源
MOLECULES | 2015年 / 20卷 / 11期
关键词
keto-enols; heterocycles; breast cancer; fungal strains; CURCUMIN; ANALOGS; INTEGRATION; INHIBITORS;
D O I
10.3390/molecules201119684
中图分类号
Q5 [生物化学]; Q7 [分子生物学];
学科分类号
071010 ; 081704 ;
摘要
Recently, a new generation of highly promising inhibitors bearing -keto-enol functionality has emerged. Reported herein is the first synthesis and use of novel designed drugs based on the -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, H-1-NMR, C-13-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 mu M. The results revealed that these compounds showed better IC50 values while compared with positive controls.
引用
收藏
页码:20186 / 20194
页数:9
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