FIELD: pharmaceutical chemistry.
SUBSTANCE: invention provides water-soluble camptotecine derivatives showing excellent therapeutical activity and retarded release suitable for cancer chemotherapy. High-molecular weight camptotecine derivative has structure wherein carboxylic acid group of block copolymer of polyethylene glycol and polymer containing carboxylic acid group in side chain and being acidic amino acid polymer is linked to phenol hydroxyl group of phenolic camptotecines through ester linkage. Also claimed is high-molecular weight camptotecine derivative of general formula (I): . Preparation method comprises combining carboxylic acid group of above-defined block copolymer with phenol hydroxyl group of phenolic camptotecines through ester linkage in presence of condensation agent. Anticancer drug includes above-defined camptotecine derivative and optionally pharmaceutically acceptable carrier.
EFFECT: augmented choice of anticancer drugs.
9 cl, 2 dwg, 2 tbl, 5 ex
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Authors
Dates
2008-01-27—Published
2003-10-29—Filed