Synthesis and pharmacokinetic property improvement of deuterated plinabulin 9
| العنوان: | Synthesis and pharmacokinetic property improvement of deuterated plinabulin 9 |
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| المؤلفون: | Huashi Guan, Hejuan Cheng, Zhongpeng Ding, Wenbao Li, Wang Shixiao, Zhiyun Meng, Guifang Dou, Jianchun Zhao, Sun Tianwen |
| المصدر: | Journal of Ocean University of China. 16:305-310 |
| بيانات النشر: | Springer Science and Business Media LLC, 2017. |
| سنة النشر: | 2017 |
| مصطلحات موضوعية: | 0301 basic medicine, Chemistry, Ocean Engineering, Total body, Pharmacology, Oceanography, Combinatorial chemistry, In vitro, 03 medical and health sciences, chemistry.chemical_compound, 030104 developmental biology, 0302 clinical medicine, Deuterium, Pharmacokinetics, In vivo, 030220 oncology & carcinogenesis, Blood circulation, Derivative (chemistry), Plinabulin |
| الوصف: | Plinabulin, a potent microtubule-targeting agent, is derived from marine natural diketopiperazine ‘phenylahistin’. To develop novel plinabulin analogue that could display better pharmacokinetic properties and less side effects, deuterated plinabulin 9 was synthesized and evaluated in vitro and in vivo. In comparison with plinabulin, in vivo pharmacokinetic studies indicated that the deuterated derivative 9 could alter blood circulation behavior obviously, which was proved by increased area under the plasma concentration- time curve (AUC0–∞), reduced clearance (CL), and prolonged total body mean residence time (MRT). The derivative 9 also has higher inhibition rates against BxPC-3, Jurkat and A-431 tumor cell lines as compared with its prototype plinabulin. Therefore, the deuterated compound 9 might be developed as a potential agent for different cancer treatments. |
| تدمد: | 1993-5021 1672-5182 |
| URL الوصول: | https://explore.openaire.eu/search/publication?articleId=doi_________::4c0ab4fae7b6687f70d40f1bcb941797 https://doi.org/10.1007/s11802-017-3177-z |
| حقوق: | CLOSED |
| رقم الأكسشن: | edsair.doi...........4c0ab4fae7b6687f70d40f1bcb941797 |
| قاعدة البيانات: | OpenAIRE |
Find this article in full text from Springer Verlag. | تدمد: | 19935021 16725182 |
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