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Synthesis of Benzophenones and in?vitro Evaluation of Their Anticancer Potential in Breast and Prostate Cancer Cells |
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| Authors: | Lydia Saidi Dr Djenisa H A Rocha Dr Oualid Talhi Dr Yamina Bentarzi Prof?Dr Bellara Nedjar-Kolli Dr Khaldoun Bachari Dr Filipe A Almeida?Paz Dr Luisa A Helguero Prof?Dr Artur M S Silva |
| Affiliation: | 1. Laboratory of Applied Organic Chemistry, Faculty of Chemistry, Houari Boumediene University of Sciences and Technology, USTHB, BP 32, El-Alia, Bab-Ezzouar, 16111 Algiers, Algeria
These authors contributed equally to this work.;2. QOPNA and LAQV-REQUIMTE, Department of Chemistry, University of Aveiro, 3810-193 Aveiro, Portugal;3. Laboratory of Applied Organic Chemistry, Faculty of Chemistry, Houari Boumediene University of Sciences and Technology, USTHB, BP 32, El-Alia, Bab-Ezzouar, 16111 Algiers, Algeria;4. Centre de Recherche Scientifique et Technique en Analyses Physico-Chimiques (CRAPC), BP384, Bou-Ismail, 42004 Tipaza, Algeria;5. CICECO-Aveiro Institute of Materials, University of Aveiro, 3810-193 Aveiro, Portugal;6. Institute of Biomedicine (iBiMED), Department of Medical Sciences, University of Aveiro, 3810-193 Aveiro, Portugal |
| Abstract: | Breast and prostate cancers are frequently treated with chemotherapy. Several novel chemicals are being reported for this purpose, particularly synthetic and natural benzophenones. This work reports the synthesis of substituted 2-hydroxybenzophenones through 1,4-conjugate addition/intramolecular cycloaddition/dehydration of nitromethane on key intermediate chromones. Structures were extensively studied by means of 2D NMR spectroscopy and single-crystal XRD. Their cytotoxicity was evaluated in vitro in two breast cancer cell lines (MDA-MB-231 and T47-D) and one prostate cancer cell line (PC3). The most potent compound exhibited good cytotoxic effects against the three cancer cell lines (IC50 values ranging from 12.09 to 26.49 μm ) and induced cell-cycle retardation only on prostate cancer cells, which suggested that it might exert cell-type-specific effects. |
| Keywords: | benzophenones cancer cytotoxicity drug design synthesis design |