Three Component One-Pot Synthesis and Antiproliferative Activity of New [1,2,4]Triazolo[4,3-<i>a</i>]pyrimidines
Manel Ben Hassen,
Dhouha Msalbi,
Badr Jismy,
Fares Elghali,
Sami Aifa,
Hassan Allouchi,
Mohamed Abarbri,
Fakher Chabchoub
Affiliations
Manel Ben Hassen
Laboratory of Applied Chemistry: Heterocycles, Lipids, and Polymers, Faculty of Sciences of Sfax, University of Sfax, Sfax 3000, Tunisia
Dhouha Msalbi
Laboratory of Molecular and Cellular Screening Processes, Centre of Biotechnology of Sfax, Sfax 3018, Tunisia
Badr Jismy
Laboratory of Physico-Chemistry of Materials and Electrolytes for Energy (PCM2E), Faculty of Science and Technology, University of Tours, 37200 Tours, France
Fares Elghali
Laboratory of Molecular and Cellular Screening Processes, Centre of Biotechnology of Sfax, Sfax 3018, Tunisia
Sami Aifa
Laboratory of Molecular and Cellular Screening Processes, Centre of Biotechnology of Sfax, Sfax 3018, Tunisia
Hassan Allouchi
Faculty of Pharmacy, University of Tours, 37200 Tours, France
Mohamed Abarbri
Laboratory of Physico-Chemistry of Materials and Electrolytes for Energy (PCM2E), Faculty of Science and Technology, University of Tours, 37200 Tours, France
Fakher Chabchoub
Laboratory of Applied Chemistry: Heterocycles, Lipids, and Polymers, Faculty of Sciences of Sfax, University of Sfax, Sfax 3000, Tunisia
A series of new [1,2,4]triazolo[4,3-a]pyrimidine derivatives was prepared using a one-pot three-component synthesis from 5-amino-1-phenyl-1H-1,2,4-triazoles, aromatic aldehydes and ethyl acetoacetate. The compound structures were confirmed by IR, 1H-NMR, 13C-NMR, HRMS and X-ray analyses. The biological activity of these compounds as antitumor agents was evaluated. Their antitumor activities against cancer cell lines (MDA-MB-231 and MCF-7) were tested by the MTT in vitro method. Among them, compounds 4c and 4j displayed the best antitumor activity with IC50 values of 17.83 μM and 19.73 μM against MDA-MB-231 and MCF-7 cell lines, respectively, compared to the Cisplatin reference.
