Synthesis and biological evaluation of novel C6-amino substituted 4-azasteroidal purine nucleoside analogues |
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| Affiliation: | 1. College of Chemistry and Molecular Engineering, Zhengzhou University, Zhengzhou 450001, China;2. School of Pharmaceutical Sciences, Zhengzhou University, Zhengzhou 450001, China;3. New Drug Research & Development Center, Zhengzhou University, Zhengzhou 450001, China;1. Mental Health Institute of The Second Xiangya Hospital, National Technology Institute of Psychiatry, Key Laboratory of Psychiatry and Mental Health of Hunan Province, Central South University, Changsha, Hunan 410011, China;2. Wuxi Mental Health Center of Nanjing Medical University, Wuxi, Jiangsu, China;3. Unit on Statistical Genomics, Intramural Research Program, National Institute of Mental Health, National Institutes of Health, Bethesda, Maryland, United States;1. Department of Chemical Physiology, The Scripps Research Institute, 10550 N. Torrey Pines Road, La Jolla, CA 92037, USA;1. Univ Paris Sud, Orsay F-91405, France;2. UMR 176, Institut Curie/CNRS, Bât. 110-112, Centre Universitaire, 91405 Orsay, France;1. Department of Chemistry, University of Alberta, 11227 Saskatchewan Drive, Edmonton, Alberta T6G 2G2, Canada;2. Swiss Center for Applied Human Toxicology and Division of Molecular and Systems Toxicology, Department of Pharmaceutical Sciences, University of Basel, Klingelbergstrasse 50, CH-4056 Basel, Switzerland;1. Nuclear Medicine Division, TRIUMF, Vancouver V6T 2A3, Canada;2. Diagnostics and Biomedical Technologies, GE Global Research, Niskayuna, NY 12309, USA;3. Department of Physics and Astronomy, University of British Columbia, Vancouver V6T 1Z1, Canada;4. Centre of Excellence for Functional Cancer Imaging, British Columbia Cancer Agency, Vancouver V5Z 4E6, Canada;5. Department of Radiology, Faculty of Medicine, University of British Columbia, Vancouver V5C 1M9, Canada;6. Experimental Therapeutics, British Columbia Cancer Agency, Vancouver V5Z 4E6, Canada;7. Division of Pharmaceutics and Biopharmaceutics, Faculty of Pharmacy, University of British Columbia, Vancouver V6T 1Z3, Canada |
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| Abstract: | Novel C6-amino substituted purine nucleoside analogues (2–12) bearing a modified pyranose-like D ring of the 4-azasteroid moiety were efficiently synthesized through nucleophilic substitution at C6 position of the steroidal nucleoside precursors (1a, b) with versatile amines. All the synthesized new compounds were evaluated for their anticancer activity in vitro against Hela, PC-3 and MCF-7 cell lines. Among them, compounds 4b, 7b and 9b exhibited significant cytotoxicity with the IC50 values of 2.99 μM (PC-3), 2.84 μM, (PC-3) and 2.69 μM (Hela), respectively. |
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| Keywords: | 4-Azasteroid Purine Nucleoside analogues Amines Anticancer activity |
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