Design,synthesis and preliminary bioactivity studies of 1,2-dihydrobenzo[d]isothiazol-3-one-1,1-dioxide hydroxamic acid derivatives as novel 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 Rd, Ji’nan 250012, PR China;2. Division of Pharmaceutical Sciences, School of Pharmacy, University of Wisconsin, Madison 53705, USA;3. Cyrus Tang Hematology Center, Soochow University, Suzhou, China 215123;4. Institute of Functional Nano & Soft Materials, Soochow University, Suzhou, China 215123;5. Department of Pharmacology, Pharmacy School, Soochow University, Suzhou, China 215123;6. Jiangsu Institute of Hematology, First Affiliated Hospital of Soochow University, Suzhou, China 215006;1. Department of Chemistry, Government College University, Faisalabad, 38000, Pakistan;2. Centre for Advanced Drug Research, COMSATS Institute of Information Technology, Abbottabad, 22060, Pakistan;3. Department of Chemistry, Government College Women University, Faisalabad, 38000, Pakistan;4. Faculty of Pharmacy, Universiti Teknologi MARA, Puncak Alam Campus, 42300 Bandar Puncak Alam, Selangor Darul Ehsan, Malaysia;5. Atta-ur-Rahman Institute for Natural Products Discovery (AuRIns), Universiti Teknologi MARA, Puncak Alam Campus, 42300 Bandar Puncak Alam, Selangor Darul Ehsan, Malaysia;6. Drug Discovery and Structural Biology Group, Health Biotechnology Division, National Institute for Biotechnology and Genetic Engineering, Faisalabad 38000, Pakistan;1. Genextra Group, Congenia Srl, Genextra Group, Via Adamello 16, 20139 Milan, Italy;2. Drug Discovery Program, Department of Experimental Oncology, European Institute of Oncology, Via Adamello 16, 20139 Milan, Italy;3. Genextra Group, DAC Srl, Genextra Group, Via Adamello 16, 20139 Milan, Italy;4. NiKem Research Srl, Via Zambeletti 25, 20021 Baranzate, MI, Italy;5. European Institute of Oncology, Via Adamello 16, 20139 Milan, Italy;6. University of Milan, University of Milan, Via Celoria 26, 20133 Milan, Italy |
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| Abstract: | Histone deacetylase (HDAC) is a clinically validated target for antitumor therapy. In order to increase HDAC inhibition and efficiency, we developed a novel series of saccharin hydroxamic acids as potent HDAC inhibitors. Among them, compounds 11e, 11m, 11p exhibited similar or better HDACs inhibitory activity compared with the approved drug SAHA. Further biological evaluation indicated that compound 11m had potent antiproliferative activities against MDA-MB-231 and PC-3. |
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| Keywords: | Histone deacetylase inhibitor Antiproliferative |
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