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Open AccessArticle

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

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Department of Chemistry, Faculty of Sciences, University Mohamed I, Oujda-60000, Morocco
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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
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Molecules, Solids and Reactivity (MOST), Institute of Condensed Mater and Nanosciences (IMCN), Université catholique de Louvain (UCL), Place Louis Pasteur 1, Louvain-la-Neuve 1348, Belgium
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Department of Biologie, Faculty of Sciences, University Mohamed I, Oujda-60000, Morocco
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Department of Chemistry, Faculty of Science, King Saud University, P. O. Box 2455, Riyadh 11451, Saudi Arabia
*
Author to whom correspondence should be addressed.
Academic Editor: Richard A. Bunce
Molecules 2015, 20(11), 20186-20194; https://doi.org/10.3390/molecules201119684
Received: 4 September 2015 / Revised: 30 October 2015 / Accepted: 2 November 2015 / Published: 10 November 2015
(This article belongs to the Collection Heterocyclic Compounds)
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, 13C-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. View Full-Text
Keywords: keto-enols; heterocycles; breast cancer; fungal strains keto-enols; heterocycles; breast cancer; fungal strains
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MDPI and ACS Style

Radi, S.; Tighadouini, S.; Feron, O.; Riant, O.; Bouakka, M.; Benabbes, R.; Mabkhot, Y.N. Synthesis of Novel β-Keto-Enol Derivatives Tethered Pyrazole, Pyridine and Furan as New Potential Antifungal and Anti-Breast Cancer Agents. Molecules 2015, 20, 20186-20194.

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