Synthesis of a Natural Chalcone and Its Prenyl Analogs – Evaluation of Tumor Cell Growth‐Inhibitory Activities,and Effects on Cell Cycle and Apoptosis |
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| Authors: | Marta P Neves Raquel T Lima Kanthima Choosang Panee Pakkong Maria de?São?José?Nascimento M Helena Vasconcelos Madalena Pinto Artur M S Silva Honorina Cidade |
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| Institution: | 1. Centro de Química Medicinal da Universidade do Porto (CEQUIMED‐UP), Rua Aníbal Cunha, 164, PT‐4050‐047 Porto (phone: +351‐222‐078916;2. fax: +351‐222‐003977);3. Laboratório de Química Organica e Farmacêutica, Departamento de Ciências Químicas, Faculdade de Farmácia, Universidade do Porto, Rua Aníbal Cunha, 164, PT‐4050‐047 Porto;4. IPATIMUP – Instituto de Patologia e Imunologia Molecular da Universidade do Porto, Rua Dr. Roberto Frias s/n, PT‐4200‐465 Porto;5. Inter Departmental Multidisciplinary Graduate Program in Bioscience, Faculty of Science, Kasetsart University, Bangkok 10900, Thailand;6. Applied Radiation and Isotopes Department, Faculty of Science, Kasetsart University, Bangkok 10900, Thailand;7. Laboratório de Microbiologia, Departamento de Ciências Biológicas, Faculdade de Farmácia, Universidade do Porto, Rua Aníbal Cunha 164, PT‐4050‐047 Porto;8. Departamento de Química & QOPNA, Universidade de Aveiro, Campus Universitário de Santiago, PT‐3810‐193 Aveiro |
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| Abstract: | Six prenyl (=3‐methylbut‐2‐en‐1‐yl) chalcones (=1,3‐diphenylprop‐2‐en‐1‐ones), 2 – 7 , and one natural non‐prenylated chalcone, 1 , have been synthesized and evaluated for their in vitro growth‐inhibitory activity against three human tumor cell lines. A pronounced dose‐dependent growth‐inhibitory effect was observed for all prenylated derivatives, except for 7 . The chalcone possessing one prenyloxy group at C(2′), i.e., 2 , was the most active derivative against the three human tumor cell lines (5.9<GI50<7.7 μM ). The majority of compounds caused an increase in percentage of apoptotic cells and/or they interfered with cell cycle distribution in the MCF‐7 cell line. |
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| Keywords: | Chalcones prenyl‐ Antitumor activity Inhibitors |
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