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

…, JS Driscoll, JS Roth, RL Heideman…

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

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Citation Number: 3

Abstract

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 ...