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Spiromustine analogues. Relationships between structure, plasma stability, and antitumor activity

…, JS Driscoll, JS Roth, RL Heideman…

文献索引:Haces; Driscoll; Roth; Heideman; Kelley Journal of Pharmaceutical Sciences, 1986 , vol. 75, # 3 p. 313 - 316

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被引用次数: 3

摘要

Abstract Spiromustine is a hydantoin-containing nitrogen mustard currently in Phase I clinical trial. Since the in vitro plasma half-life of this compound (6.4 min, 37 C, pH 7.4) appeared to be influenced by the hydantoin ring, analogues containing 2–5 methylene spacer groups between this ring and the nitrogen mustard moiety were prepared and evaluated for hydrolytic stability and antitumor activity. Stability correlated with structure ...