Novel inhibitors of human histone deacetylases: Design,synthesis and bioactivity of 3-alkenoylcoumarines |
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| Institution: | 1. Laboratoire de Biologie Moléculaire et Cellulaire du Cancer, Hôpital Kirchberg, L-2540 Luxembourg, Luxembourg;2. UMR CNRS 7565 SRSMC, Université de Lorraine, 57070 Metz, France;3. Dipartimento di Chimica e Tecnologie del Farmaco, Sapienza Università di Roma, P.le Aldo Moro 5, 00185 Roma, Italy;4. Department of Pharmacy, College of Pharmacy, Seoul National University, Building 20 Room 303, 1 Gwanak-ro, Gwanak-gu, Seoul 151-742, Republic of Korea;1. Centro de Química Medicinal – Universidade do Porto (CEQUIMED-UP), Departamento de Ciências Químicas, Faculdade de Farmácia, Universidade do Porto, Rua Jorge Viterbo Ferreira n° 228, 4050-313 Porto, Portugal;2. Laboratório de Química Orgânica e Farmacêutica, Departamento de Ciências Químicas, Faculdade de Farmácia, Universidade do Porto, Rua Jorge Viterbo Ferreira n° 228, 4050-313 Porto, Portugal;3. Cancer Drug Resistance Group, IPATIMUP – Institute of Molecular Pathology and Immunology of the University of Porto, Rua Dr. Roberto Frias, S/N, 4200-465 Porto, Portugal;4. Centro de Investigação em Ciências da Saúde (CICS), Instituto Superior de Ciências da Saúde – Norte, CESPU, Rua Central de Gandra 1317, 4585-116 Gandra PRD, Portugal;5. Laboratório de Tecnologia Farmacêutica, Departamento de Ciências do Medicamento, Faculdade de Farmácia, Universidade do Porto, Portugal;6. Laboratório de Microbiologia, Departmento de Ciências Biológicas, Faculdade de Farmácia, Universidade do Porto, Portugal |
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| Abstract: | Histone deacetylases (HDACs) are well-established, promising targets for anticancer therapy due to their critical role in cancer development. Accordingly, an increasing number of HDAC inhibitors displaying cytotoxic effects against cancer cells have been reported. Among them, a large panel of chemical structures was described including coumarin-containing molecules. In this study, we described synthesis and biological activity of new coumarin-based derivatives as HDAC inhibitors. Among eight derivatives, three compounds showed HDAC inhibitory activities and antitumor activities against leukemia cell lines without affecting the viability of peripheral blood mononuclear cells from healthy donors. |
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| Keywords: | Chalcone Coumarin Histone deacetylase inhibitors Anti-proliferative activity Cancer |
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