Novel oxa-spermine homologues: synthesis and cytotoxic properties.
New oxa-spermine homologues 5-9 were synthesised and their anticancer properties were evaluated against a broad spectrum of cancer cells. All compounds, except 9 showed average GI(50) values in the range of 1.89-7.56 microM. SAR studies showed that the cytotoxic activity of these novel oxa-spermines depended on the length of the alkyl chain, the position of the oxa-amino functionality and also, on the type of sulphonamido group in the molecule. Although the mechanism of action of these compound remains to be elucidated, it would appear that direct drug-DNA interactions are not involved in the mode of action of these drugs.
Kuksa
Vladimir A
VA
Department of Ophthalmology, School of Medicine, University of Washington, 1957 NE Pacific Avenue, Seattle, WA 98195-6485, USA.
Pavlov
Valentin A
VA
Kong Thoo Lin
Paul
P
D000818:Animals; D000970:Antineoplastic Agents / Q000138:chemical synthesis* / Q000378:metabolism / Q000494:pharmacology; D002470:Cell Survival / Q000187:drug effects; D004247:DNA / Q000378:metabolism; D004354:Drug Screening Assays, Antitumor; D020128:Inhibitory Concentration 50; D009928:Organ Specificity; D013096:Spermine / Q000031:analogs & derivatives* / Q000138:chemical synthesis / Q000494:pharmacology; D013329:Structure-Activity Relationship; D013696:Temperature; D014407:Tumor Cells, Cultured
D000970:Antineoplastic Agents; D013096:Spermine; D004247:DNA; C427203:calf thymus DNA