Novel lipid analogs with cytostatic and cytocidal activity.
1-0-Alkyl diol and glyceryl ether lipids with a quaternary ammonium polar head group were synthesized and the cytotoxicity (IC50) tested against KB cells, with low 1-0-alkyl-cleavage activity, and rat hepatoma 77 cells with relatively high 1-0-alkyl-cleavage activity. The original premise was that the compounds would be inactivated by the cleavage enzyme and thus be selectively toxic to cells with less of the enzyme. Results with two other cell lines with equivalent cleavage enzyme, HL-60 and K562-4, however, are not consistent with this premise.
Crumpton
S C
SC
Division of Medicinal Chemistry, School of Pharmacy, University of North Carolina, Chapel Hill 27514.
Goz
B
B
Ishaq
K S
KS
D000818:Animals; D000970:Antineoplastic Agents / Q000138:chemical synthesis* / Q000494:pharmacology; D002455:Cell Division / Q000187:drug effects*; D002460:Cell Line; D002470:Cell Survival / Q000187:drug effects*; D004075:Diglycerides / Q000138:chemical synthesis* / Q000494:pharmacology; D005989:Glycerides / Q000138:chemical synthesis*; D005995:Glyceryl Ethers / Q000138:chemical synthesis* / Q000494:pharmacology; D006801:Humans; D007624:KB Cells; D051381:Rats; D013329:Structure-Activity Relationship
D000970:Antineoplastic Agents; D004075:Diglycerides; D005989:Glycerides; D005995:Glyceryl Ethers