Synthesis of deuterium-enriched and fluorine-substituted plinabulin derivatives and evaluation of their antitumor activities |
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Authors: | Zhongpeng Ding Yingwei Hou Shixiao Wang Tianwen Sun Mingxu Ma Huashi Guan Wenbao Li |
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Affiliation: | 1.Key Laboratory of Marine Drugs of Ministry of Education of China, School of Medicine and Pharmacy,Ocean University of China,Qingdao,People’s Republic of China;2.Marine Biomedical Research Institute of Qingdao,Qingdao,People’s Republic of China |
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Abstract: | Deuterium-enriched and fluorine-substituted compounds have been widely applied in drug discovery due to their advantages in the studies of clinical pharmacokinetics and metabolic profiles. Herein we synthesized a library of deuterated and fluorine-substituted plinabulin derivatives, and all 15 D- or F-compounds were characterized by MS, (^{1}hbox {H}) NMR and (^{ 13}hbox {C},hbox {NMR}). Their antitumor activities were evaluated against human Jurkat T lymphocyte cells. |
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