期刊
CHEMICAL & PHARMACEUTICAL BULLETIN
卷 60, 期 7, 页码 877-881出版社
PHARMACEUTICAL SOC JAPAN
DOI: 10.1248/cpb.c12-00216
关键词
water-soluble prodrug; anti-microtubule agent; click chemistry; plinabulin; monolactim
资金
- MEXT (Ministry of Education, Culture, Sports, Science and Technology) of Japan [20390036, 21890262, 21790118]
- Grants-in-Aid for Scientific Research [23790143, 23390029, 20390036, 21890262, 21790118] Funding Source: KAKEN
Plinabulin (1) is a potent anti-microtubule agent, however, its low water solubility has to be improved for the advantage in pharmacokinetics and chemotherapy. In this report, the replaceable water-solubilizing moiety of the water-soluble prodrug of plinabulin (1) was investigated. The properties of the water-soluble prodrugs of plinabulin (1), in which the water-solubilizing part was replaced with a new functionality, were evaluated. The newly introduced water-solubilizing moiety provided interesting effects on the water solubility and half-life of the prodrugs.
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