One-Pot Synthesis and Antiproliferative Activity of Highly Functionalized Pyrazole Derivatives |
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Authors: | Dr Matteo Lusardi Dr Chiara Rotolo Dr Marco Ponassi Dr Erika Iervasi Dr Camillo Rosano Prof Andrea Spallarossa |
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Affiliation: | 1. Department of Pharmacy, University of Genova, viale Benedetto XV, 3, 16132 Genova, Italy;2. Proteomics and Mass Spectrometry Unit, IRCCS Ospedale Policlinico San Martino, Largo R. Benzi 10, 16132 Genova, Italy |
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Abstract: | A series of highly functionalized pyrazole derivatives has been prepared by a one-pot, versatile and regioselective procedure. Pyrazoles 1 – 29 were tested in cell-based assay to assess their antiproliferative activity against a panel of tumour cells. Additionally, the cytotoxicity of prepared compounds was evaluated against normal human fibroblasts. The antiproliferative activity of the synthesized molecules emerged to be affected by the nature of the substituents of the pyrazole scaffold and derivatives 21 – 23 proved to inhibit the growth of melanoma and cervical cancer cells. Compound 23 was identified as the most active derivative and docking simulations predicted its ability to interact with estrogen receptors. |
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Keywords: | one-pot synthesis pyrazole derivatives antiproliferative agents docking simulations |
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