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Synthesis of deuterium-enriched and fluorine-substituted plinabulin derivatives and evaluation of their antitumor activities
Authors:Zhongpeng Ding  Yingwei Hou  Shixiao Wang  Tianwen Sun  Mingxu Ma  Huashi Guan  Wenbao Li
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
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.
Keywords:
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