Synthesis and in vivo antitumor activity of poly(L-glutamic acid) conjugates of 20(S)-camptothecin

被引：118

作者：

Bhatt, RL ^{[1
]}

de Vries, P ^{[1
]}

Tulinsky, J ^{[1
]}

Bellamy, G ^{[1
]}

Baker, B ^{[1
]}

Singer, JW ^{[1
]}

Klein, P ^{[1
]}

机构：

[1] Cell Therapuet Inc, Seattle, WA 98119 USA

来源：

JOURNAL OF MEDICINAL CHEMISTRY | 2003年 / 46卷 / 01期

关键词：

D O I：

10.1021/jm020022r

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

Poly-alpha-(L-glutamic acid) (PG) conjugates of 20(S)-camptothecin (1, CPT) displayed improved aqueous solubility compared to CPT, were stable in aqueous solution at neutral pH, and were potent antitumor agents in vivo. Evaluation of PG molecular weight, CPT loading, aqueous solubility, and CPT equivalent dosing with respect to in vivo antitumor potencies of various linked conjugates led to identification of a preferred conjugate composition.

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页码：190 / 193

页数：4

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