SYNTHESIS AND ANTITUMOR ACTIVITY OF SPERGUALIN ANALOGUES: II. CHEMICAL MODIFICATION OF THE SPERMIDINE MOIETY

Chemical modifications of the spermidine moiety of an antitumor antibiotic, spergualin (Ia), and the structure-activity relationship are described. Replacement of spermidine with other poly amines decreased the antitumor activity against mouse leukemia LI 210. Analogues containing an oxidized spermi...

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Veröffentlicht in:	Journal of antibiotics 1987/09/25, Vol.40(9), pp.1303-1315
Hauptverfasser:	UMEDA, YOSHIHISA, MORIGUCHI, MAKOTO, KURODA, HIROYUKI, NAKAMURA, TERUYA, FUJII, AKIO, IINUMA, HIRONOBU, TAKEUCHI, TOMIO, UMEZAWA, HAMAO
Format:	Artikel
Sprache:	eng
Schlagworte:	Aliphatic compounds Animals Antibiotics, Antineoplastic - chemical synthesis Antibiotics, Antineoplastic - therapeutic use Chemistry Exact sciences and technology Guanidines - chemical synthesis Guanidines - therapeutic use Leukemia L1210 - drug therapy Male Mice Organic chemistry Preparations and properties Spermidine - analysis Structure-Activity Relationship
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Zusammenfassung:	Chemical modifications of the spermidine moiety of an antitumor antibiotic, spergualin (Ia), and the structure-activity relationship are described. Replacement of spermidine with other poly amines decreased the antitumor activity against mouse leukemia LI 210. 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.
ISSN:	0021-8820 1881-1469
DOI:	10.7164/antibiotics.40.1303