期刊
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
卷 15, 期 15, 页码 3576-3579出版社
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmcl.2005.05.057
关键词
doxorubicin; phosphazene trimer; antitumor agent; tetrapeptide
A new biodegradable water-soluble phosphazene trimer-doxorubicin conjugate was synthesized, in which equimolar hydrophilic methoxy-poly(ethylene glycol) with a molecular weight of 350 (MPEG350) and a tumor-specific tetrapeptide (Gly-Phe-Leu-Gly) were grafted to cyclotriphosphazene. The present conjugate exhibited cytotoxicity lower than that of free doxorubicin (IC50 = 0.10 mu M) but a reasonably higher in vitro cytotoxicity (IC50 = 1.1 mu M) against the leukemia L1210 cell line probably due to its enzymatically controlled release. (c) 2005 Elsevier Ltd. All rights reserved.
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