Synthesis and anti-tumor activity of glycosyl oxadiazoles derivatives |
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| Institution: | 1. Department of Cardiology, Royal North Shore Hospital, Sydney, NSW, Australia;2. Department of Medicine, Population Health Research Institute, Hamilton Health Sciences, McMaster University, Hamilton, Ontario, Canada;1. N.D. Zelinsky Institute of Organic Chemistry, Russian Academy of Sciences, 47 Leninsky Prosp., 119991 Moscow, Russian Federation;2. A.N. Nesmeyanov Institute of Organoelement Compounds, Russian Academy of Sciences, 28 Vavilov St., 119991 Moscow, Russian Federation;1. College of Biotechnology and Pharmaceutical Engineering, Nanjing University of Technology, 30 Puzhunan Road, Nanjing 211816, People''s Republic of China;2. College of Pharmaceutical Science, Nanjing University of Chinese Medicine, Nanjing 210046, Jiangsu, People''s Republic of China;1. Department of Chemistry, Laboratory of Organic Chemistry, Aristotle University of Thessaloniki, University Campus, Thessaloniki 54124, Macedonia, Greece;2. Department of Pharmaceutical Chemistry, School of Pharmacy, Aristotle University of Thessaloniki, Thessaloniki 54124, Macedonia, Greece;3. Institute of Nanotechnology, Karlsruhe Institute of Technology, Hermann-von-Helmholtz Platz 1, 76344 Eggenstein-Leopoldshafen, Germany |
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| Abstract: | A new series of glycosyl oxadiazoles compounds were synthesized and characterized through 1H NMR, 13C NMR, IR and HRMS. The anti-tumor activities for MDA-MB-231 of all these new compounds were screened in vitro by MTT assay. Due to the modification of gastrodin analogues, the anti-tumor activities of these 1,3,4-oxadiazoles derivatives were greatly improved. Six compounds (6c, 6d, 6i, 6j, 6k and 6l) displayed relatively higher MDA-MB-231 potency with IC50 values (0.89, 0.26, 1.35, 3.60, 0.95 and 1.08 μM) compared with the reference medicine Rosiglitazone (5.23 μM). |
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| Keywords: | Gastrodin analogues Anti-tumor activities Oxadiazoles derivatives Heterocycles |
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