Synthesis and antitumor activities of amino acid prodrugs of amino-combretastatins

Authors: Ohsumi K.; Hatanaka T.; Nakagawa R.; Fukuda Y.; Morinaga Y.; Suga Y.; Nihei Y.; Ohishi K.; Akiyama Y.; Tsuji T.

Source: Anti-Cancer Drug Design, Volume 14, Number 6, 1999 , pp. 539-548(10)

Publisher: Cognizant Communication Corporation

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Abstract:

The synthesis and antitumor activity of water-soluble amino acid prodrugs of amino-combretastatins were reported. Among the synthesized compounds, 7e (CS-39-L--SerlHCl, AC-7700) showed enhanced antitumor activity and decreased toxicity in a Colon 26 murine adenocarcinoma model. Compound 7e showed improved solubility and was easily formulated for in vivo administration. Compound 7e was cleaved to generate the parent compound, CS-39, in the whole blood of mice as well as man, possibly by the action of amino peptidase on the erythrocyte membrane.

Keywords: A-4; CS-28.HCl; CS-39.HCl; CS-39-

Document Type: Research article

Affiliations: 1: Corresponding author

Publication date: 1999-12-01