氘代和氟取代普兰布林衍生物的合成及其抗肿瘤活性评价。
Synthesis of deuterium-enriched and fluorine-substituted plinabulin derivatives and evaluation of their antitumor activities.
机构信息
Key Laboratory of Marine Drugs of Ministry of Education of China, School of Medicine and Pharmacy, Ocean University of China, Qingdao, 266003, People's Republic of China.
Marine Biomedical Research Institute of Qingdao, Qingdao, 266071, People's Republic of China.
出版信息
Mol Divers. 2017 Aug;21(3):577-583. doi: 10.1007/s11030-017-9742-y. Epub 2017 May 9.
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, [Formula: see text] NMR and [Formula: see text]. Their antitumor activities were evaluated against human Jurkat T lymphocyte cells.
氘代和氟取代化合物由于在临床药代动力学和代谢谱研究中的优势，已被广泛应用于药物发现。在此，我们合成了一系列氘代和氟取代的普林司他衍生物，所有 15 种 D-或 F-化合物均通过 MS、[Formula: see text] NMR 和 [Formula: see text] 进行了表征。并对它们在人 Jurkat T 淋巴细胞中的抗肿瘤活性进行了评估。
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