Design and synthesis of a new generation of substituted purine hydroxamate analogs as histone deacetylase inhibitors |
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| Institution: | 1. Department of Medicinal Chemistry, Key Laboratory of Chemical Biology (Ministry of Education), School of Pharmacy, Shandong University, 44 West Wenhua Road, Ji’nan, Shandong 250012, PR China;2. School of Pharmacy, University of Wisconsin-Madison, Madison 53705, USA;1. Inserm, U892, Nantes F-44000, France;2. CNRS, UMR 6299, Nantes F-44000, France;3. University of Nantes, Nantes F-44000, France;4. Laboratoire de Chimie des Polymères Organiques, CNRS, UMR 5629, Bordeaux, 16 Avenue Pey-Berland, F-33607 Pessac, France;5. Institut de Chimie des Milieux et Matériaux de Poitiers, CNRS, UMR 7285, Poitiers. 4, Rue Michel Brunet, TSA 51106, B27 86073 Poitiers Cedex 9, France;1. Department of Food, Environmental and Nutritional Sciences, Division of Chemistry and Molecular Biology, University of Milan, via Celoria 2, 20133 Milan, Italy;2. School of Pharmaceutical Sciences, University of Geneva, University of Lausanne, Quai Ernest-Ansermet 30, 1211 Geneva 11, Switzerland;3. Fondazione IRCCS Istituto Nazionale Tumori, Via Amadeo 42, 20133 Milano, Italy;4. R&D Sigma-Tau Industrie Farmaceutiche Riunite S.p.A., Via Pontina Km 30,400, I-00071 Pomezia, Roma, Italy;1. Department of Food, Environmental and Nutritional Sciences, Division of Chemistry and Molecular Biology, Università di Milano, Via Celoria 2, 20133 Milano, Italy;2. R&D Sigma-Tau Industrie Farmaceutiche Riunite S.p.A., Via Pontina Km 30,400, I-00040 Pomezia, RM, Italy;3. Molecular Pharmacology Unit, Dept. Experimental Oncology and Molecular Medicine, Fondazione IRCCS Istituto Nazionale Tumori, Via Amadeo 42, I-20133 Milan, Italy;1. School of Pharmacy, Nanjing University of Chinese Medicine, 138 Xianlin Road, Nanjing 210023, China;2. Jiangsu Collaborative Innovation Center of Chinese Medicinal Resources Industrialization, Nanjing 210023, Jiangsu, China;3. Pharmacy, Nanjing General Hospital, 305 Zhongshan East Road, Nanjing 210002, China;4. Jiangsu Key Laboratory for Functional Substance of Chinese Medicine, Stake Key Laboratory Cultivation Base for TCM Quality and Efficacy, School of Pharmacy, Nanjing University of Chinese Medicine, Nanjing, China |
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| Abstract: | Histone deacetylase inhibitors have been proved to be great potential for the treatment of cancer. Recently, we designed and modified a series of substituted purine hydroxamate analogs as potent HDAC inhibitors based on our previous studies. The target compounds were investigated for their in vitro HDAC inhibitory activities and anti-proliferative activities. Results indicated that these compounds could effectively inhibit HDAC and possess obvious anti-proliferative activity against tumor cells. Promisingly, target compounds 4m and 4n outperformed SAHA in both enzymatic inhibitory activity and cellular anti-proliferative activity assay. |
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| Keywords: | Purine Histone deacetylase Inhibitor Anticancer |
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