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

Authors :
Smaail Radi
Said Tighadouini
Olivier Feron
Olivier Riant
Mohammed Bouakka
Redouane Benabbes
Yahia N. Mabkhot
Source :
Molecules, Vol 20, Iss 11, Pp 20186-20194 (2015)
Publication Year :
2015
Publisher :
MDPI AG, 2015.

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.

Details

Language :
English
ISSN :
14203049
Volume :
20
Issue :
11
Database :
Directory of Open Access Journals
Journal :
Molecules
Publication Type :
Academic Journal
Accession number :
edsdoj.1c168614247a4ec5b28de971f4fa2f0f
Document Type :
article
Full Text :
https://doi.org/10.3390/molecules201119684