Synthesis and antitumor activity of novel water soluble derivatives of camptothecin as specific inhibitors of topoisomerase I

MJ Luzzio, JM Besterman, DL Emerson…

Index: Luzzio, Michael J.; Besterman, Jeffrey M.; Emerson, David L.; Evans, Michael G.; Lackey, Karen; et al. Journal of Medicinal Chemistry, 1995 , vol. 38, # 3 p. 395 - 401

Full Text: HTML

Citation Number: 150

Abstract

The synthesis and antitumor activities of the novel water soluble camptothecin derivatives 7- [(4-methylpiperazino) methylI-l0, 1 l-(methylenedioxy)-(20S)-camptothecin trifluoroacetate (6) and 7-[(4-methylpiperazino) methyll-l0, 1 l-(ethylenedioxy)-(2OS)-camptothecin trifluoroacetate (7) are described. The solubilities of compounds 6 and 7 were measured to be 4.5 and 5.8 mg/mL, respectively, in pH 5 acetate buffer in contrast to< 0.003 mg/mL for ...