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

Radi, Smaail;Tighadouini, Said;Feron, Olivier;Riant, Olivier;Mabkhot, Yahia N;et.al.
(2015) Molecules : a journal of synthetic organic and natural product chemistry — Vol. 20, n° 11, p. 20186-20194 (2015)

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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, (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.
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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 : a journal of synthetic organic and natural product chemistry, 20(11), 20186-20194. https://doi.org/10.3390/molecules201119684 (Original work published 2015)