Synthesis and in vitro evaluation of macromolecular antitumour derivatives based on phenylenediamine mustard

K De Winne, LW Seymour, EH Schacht

文献索引：De Winne, Katleen; Seymour, Leonard W.; Schacht, Etienne H. European Journal of Pharmaceutical Sciences, 2005 , vol. 24, # 2-3 p. 159 - 168

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被引用次数: 1

摘要

Poly-[N-(2-hydroxyethyl)-l-glutamine](PHEG) and poly (ethylene glycol)(PEG)-grafted PHEG conjugates of N, N-di (2-chloroethyl)-4-phenylenediamine mustard (PDM) were synthetised. A collagenase-sensitive oligopeptide spacer was selected to link the cytotoxic agent PDM onto the polymeric carrier. First, the oligopeptide-drug conjugate, l-pro-l-leu-gly-l-pro-gly- PDM, was prepared. In a second step, the low molecular weight PDM derivative and PEG- ...