Synthesis of pyrazole based novel aurone analogs and their cytotoxic activity against MCF-7 cell line

• Published in: Chemical Data Collections Vol. 30; p. 100559
• Main Authors: Kumar, Sanjeev, Lathwal, Ekta, Kumar, Gourav, Saroha, Bhavna, Kumar, Suresh, Mahata, Sutapa, Sahoo, Pranab Kumar, Nasare, Vilas D.
• Format: Journal Article
• Language: English
• Published: Elsevier B.V 01.12.2020
• Subjects: Aurone; Cytotoxic; MCF-7; Pyrazole; Solvent free; Aurone; Cytotoxic; Solvent free; MCF-7; Pyrazole
• ISSN: 2405-8300; 2405-8300
• DOI: 10.1016/j.cdc.2020.100559

•Benzofuran-3(2H)-one and pyrazole linked fourteen novel aurones were designed and synthesized under solvent free sustainable conditions.•Structures of the synthesized aurones were confirmed by their IR, 1H NMR, 13C NMR, elemental analysis and mass spectrometry data.•Cytotoxic activity of these novel hydroxy aurone derivatives was evaluated toward MCF-7 cancer cell line.•3e, 3c, 3i, 3a, and 3n displayed outstanding potency against MCF-7 (IC50: 2.7–15.5 µg/mL) in comparison to standard (paclitaxel, IC50= 18.5 µg/mL) A series of pyrazole based aurone analogs 3(a-n) have been synthesized and evaluated for their cytotoxic activity against MCF-7 cell line. All the products have been obtained by solid phase reaction and organic solvent free simple work-up procedure. Structures of the synthesized aurones were confirmed by their IR, 1H NMR, 13C NMR, elemental analysis and mass spectrometry data. The cytotoxic activity of these compounds was assessed by MTT assay and the nine products were found to be potential inhibitors against human breast adenocarcinoma cell line i.e. MCF-7. Aurone analogs 3a, 3b, 3c, 3e, 3i and 3n are the most active against the MCF-7 cell line with IC50 of 13.8, 15.8, 4.3, 2.7, 12.9 and 15.5 μg/mL respectively, as compared to paclitaxel, with an IC50 value of 18.5 μg/mL. Cytotoxicity against MCF-7 cancer cells, makes these molecules attractive candidates for the potential anticancer drug. [Display omitted]