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

Autor: Bhatt R; Cell Therapeutics, Inc., 201 Elliott Avenue West, Seattle, Washington 98119, USA., de Vries P, Tulinsky J, Bellamy G, Baker B, Singer JW, Klein P
Jazyk: angličtina
Zdroj: Journal of medicinal chemistry [J Med Chem] 2003 Jan 02; Vol. 46 (1), pp. 190-3.
DOI: 10.1021/jm020022r
Abstrakt: 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.
Databáze: MEDLINE