Synthesis and antitumor activity of spergualin analogues. II. Chemical modification of the spermidine moiety.
- 1 January 1987
- journal article
- research article
- Published by Japan Antibiotics Research Association in The Journal of Antibiotics
- Vol. 40 (9) , 1303-1315
- https://doi.org/10.7164/antibiotics.40.1303
Abstract
Chemical modifications of the spermidine moiety of an antitumor antibiotic, spergualin (Ia), and the structure-activity relationship are described. Replacement of spermidine with other polyamines decreased the antitumor activity against mouse leukemia L1210. Analogues containing an oxidized spermidine moiety that probably formed during oxidation with amine oxidase were inactive. Spermidine is indispensable for the antitumor activity. A facile method for the synthesis of glyoxyloyl polyamine, a key intermediate of spergualin-related compounds, is also reported.This publication has 2 references indexed in Scilit:
- Cytotoxicity of spergualin and amine oxidase activity in medium.The Journal of Antibiotics, 1985
- Synthesis and antitumor activity of spergualin analogues. I. Chemical modification of 7-guanidino-3-hydroxyacyl moiety.The Journal of Antibiotics, 1985