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Bioorg Med Chem. 2003 Jun 12;11(12):2635-9.

Tripartate poly(ethylene glycol) prodrugs of the open lactone form of camptothecin.

Author information

1
Enzon Inc., 20 Kingsbridge Road, Piscataway, NJ 00854, USA. richard.greenwald@enzon.com

Abstract

Two PEG prodrugs utilizing conjugation of PEG through the C-21 acid functionality as well as the C-17 OH group of CPT hydroxy-amide open forms were synthesized and characterized. Both of these open lactone tripartate prodrugs were shown to be water soluble and highly effective in MX-1 mouse xenograph studies. Indirect evidence implies that the initial ester or carbonate bond breaking is esterase mediated in the first step of the cascade of CPT release.

PMID:
12757729
DOI:
10.1016/s0968-0896(03)00152-4
[Indexed for MEDLINE]

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