Prodrug study of plinabulin using a click strategy focused on the effects of a replaceable water-solubilizing moiety.
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.
School of Pharmacy, Tokyo University of Pharmacy and Life Sciences, 1432–1 Horinouchi, Hachioji, Tokyo.
Fumika
F
Yakushiji
Hironari
H
Tanaka
Kyohei
K
Muguruma
Takahiro
T
Iwahashi
Yuri
Y
Yamazaki
Yoshio
Y
Hayashi
D054659:Diketopiperazines / Q000138:chemical synthesis / Q000737:chemistry* / Q000378:metabolism; D004950:Esterases / Q000378:metabolism; D006207:Half-Life; D006868:Hydrolysis; D011355:Prodrugs / Q000138:chemical synthesis / Q000737:chemistry* / Q000378:metabolism; D012995:Solubility; D014867:Water
D054659:Diketopiperazines; C514351:NPI 2358; D011355:Prodrugs; D014867:Water; D004950:Esterases