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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Abstract

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.

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Radi, S., Tighadouini, S., Feron, O., Riant, O., Bouakka, M., Benabbes, R., & Mabkhot, Y. N. (2015). Synthesis of novel β-keto-enol derivatives tethered pyrazole, pyridine and furan as new potential antifungal and anti-breast cancer agents. Molecules, 20(11), 20186–20194. https://doi.org/10.3390/molecules201119684

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